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Kelly Chibale - Publications

Affiliations: 
1996- University of Cape Town, Cape Town, Western Cape, South Africa 
Area:
Medicinal chemistry
Website:
http://www.kellychibaleresearch.uct.ac.za/
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240 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2023 Okombo J, Kumar M, Redhi D, Wicht KJ, Wiesner L, Egan TJ, Chibale K. Pyrido-Dibemequine Metabolites Exhibit Improved Druglike Features, Inhibit Hemozoin Formation in , and Synergize with Clinical Antimalarials. Acs Infectious Diseases. 9: 653-667. PMID 36802523 DOI: 10.1021/acsinfecdis.2c00592  0.31
2023 Byl JAW, Mueller R, Bax B, Basarab GS, Chibale K, Osheroff N. A Series of Spiropyrimidinetriones that Enhances DNA Cleavage Mediated by Gyrase. Acs Infectious Diseases. 9: 706-715. PMID 36802491 DOI: 10.1021/acsinfecdis.3c00012  0.302
2022 Singh V, Grzegorzewicz AE, Fienberg S, Müller R, Khonde LP, Sanz O, Alfonso S, Urones B, Drewes G, Bantscheff M, Ghidelli-Disse S, Ioerger TR, Angala B, Liu J, Lee RE, ... ... Chibale K, et al. 1,3-Diarylpyrazolyl-acylsulfonamides Target HadAB/BC Complex in . Acs Infectious Diseases. 8: 2315-2326. PMID 36325756 DOI: 10.1021/acsinfecdis.2c00392  0.305
2022 Kaur N, Korkor C, Mobin SM, Chibale K, Singh K. Fluorene-Chloroquine Hybrids: Synthesis, in vitro Antiplasmodial Activity, and Inhibition of Heme Detoxification Machinery of Plasmodium falciparum. Chemmedchem. e202200414. PMID 36017666 DOI: 10.1002/cmdc.202200414  0.309
2022 Berger A, Knak T, Kiffe-Delf AL, Mudrovcic K, Singh V, Njoroge M, Burckhardt BB, Gopalswamy M, Lungerich B, Ackermann L, Gohlke H, Chibale K, Kalscheuer R, Kurz T. Total Synthesis of the Antimycobacterial Natural Product Chlorflavonin and Analogs via a Late-Stage Ruthenium(II)-Catalyzed -C(sp)-H-Hydroxylation. Pharmaceuticals (Basel, Switzerland). 15. PMID 36015133 DOI: 10.3390/ph15080984  0.306
2022 Govender P, Müller R, Singh K, Reddy V, Eyermann CJ, Fienberg S, Ghorpade SR, Koekemoer L, Myrick A, Schnappinger D, Engelhart C, Meshanni J, Byl JAW, Osheroff N, Singh V, ... Chibale K, et al. Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity. Journal of Medicinal Chemistry. 65: 6903-6925. PMID 35500229 DOI: 10.1021/acs.jmedchem.2c00266  0.784
2021 Semenya D, Touitou M, Ribeiro CM, Pavan FR, Pisano L, Singh V, Chibale K, Bano G, Toscani A, Manetti F, Gianibbi B, Castagnolo D. Structural Rigidification of -Aryl-pyrroles into Indoles Active against Intracellular and Drug-Resistant Mycobacteria. Acs Medicinal Chemistry Letters. 13: 63-69. PMID 35059125 DOI: 10.1021/acsmedchemlett.1c00431  0.306
2021 Khonde LP, Müller R, Boyle GA, Reddy V, Nchinda AT, Eyermann CJ, Fienberg S, Singh V, Myrick A, Abay E, Njoroge M, Lawrence N, Su Q, Myers TG, Boshoff HIM, ... ... Chibale K, et al. 1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in . Journal of Medicinal Chemistry. PMID 34414766 DOI: 10.1021/acs.jmedchem.1c00837  0.798
2021 Mambwe D, Kumar M, Ferger R, Taylor D, Njoroge M, Coertzen D, Reader J, van der Watt M, Birkholtz LM, Chibale K. Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against In Vitro. Acs Medicinal Chemistry Letters. 12: 1333-1341. PMID 34413963 DOI: 10.1021/acsmedchemlett.1c00328  0.301
2021 Navidpour L, Chibale K, Esmaeili S, Ghiaee A, Hadjesfandiari N, Irani M, Ahmadi S, Yassa N. Antimalarial activities of ()-2-(nitroheteroarylmethylene)-3(2)-benzofuranone derivatives: , assessment and β-hematin formation inhibition activity. Antimicrobial Agents and Chemotherapy. AAC0268320. PMID 34228544 DOI: 10.1128/AAC.02683-20  0.318
2021 van der Westhuyzen R, Mabhula A, Njaria PM, Müller R, Ngumbu Muhunga D, Taylor D, Lawrence N, Njoroge M, Brunschwig C, Moosa A, Singh V, Rao SPS, Manjunatha UH, Smith PW, Warner DF, ... ... Chibale K, et al. Benzoheterocyclic Oxime Carbamates Active against : Synthesis, Structure-Activity Relationship, Metabolism, and Biology Triaging. Journal of Medicinal Chemistry. PMID 34138573 DOI: 10.1021/acs.jmedchem.1c00707  0.318
2021 Soares de Melo C, Singh V, Myrick A, Simelane SB, Taylor D, Brunschwig C, Lawrence N, Schnappinger D, Engelhart CA, Kumar A, Parish T, Su Q, Myers TG, Boshoff HIM, Barry CE, ... ... Chibale K, et al. Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies. Journal of Medicinal Chemistry. PMID 33395287 DOI: 10.1021/acs.jmedchem.0c01727  0.318
2020 Tukulula M, Louw S, Njoroge M, Chibale K. Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles. Molecules (Basel, Switzerland). 25. PMID 33333924 DOI: 10.3390/molecules25245941  0.341
2020 Cheuka PM, Centani L, Arendse LB, Fienberg S, Wambua L, Renga SS, Dziwornu GA, Kumar M, Lawrence N, Taylor D, Wittlin S, Coertzen D, Reader J, van der Watt M, Birkholtz LM, ... Chibale K, et al. New Amidated 3,6-Diphenylated Imidazopyridazines with Potent Antiplasmodium Activity Are Dual Inhibitors of Phosphatidylinositol-4-kinase and cGMP-Dependent Protein Kinase. Acs Infectious Diseases. PMID 33319990 DOI: 10.1021/acsinfecdis.0c00481  0.302
2020 Horatscheck A, Andrijevic A, Nchinda AT, Le Manach C, Paquet T, Khonde LP, Dam J, Pawar K, Taylor D, Lawrence N, Brunschwig C, Gibhard L, Njoroge M, Reader J, van der Watt M, ... ... Chibale K, et al. Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and Efficacy in the NSG Mouse Model. Journal of Medicinal Chemistry. PMID 33103428 DOI: 10.1021/acs.jmedchem.0c01411  0.346
2020 Aggarwal VK, Armstrong SK, Caggiano L, Chibale K, Clayden J, Coldham I, Greeves N, Hartley RC, Knight JG, Kuhnert N, Mitchell HJ, Nelson A, O'Brien P, Thomas SP, Wyatt P. Stuart Warren (24 Dec 1938-22 Mar 2020). Organic & Biomolecular Chemistry. PMID 32936190 DOI: 10.1039/D0Ob90121K  0.696
2020 Baartzes N, Jordaan A, Warner DF, Combrinck J, Taylor D, Chibale K, Smith GS. Antimicrobial evaluation of neutral and cationic iridium(III) and rhodium(III) aminoquinoline-benzimidazole hybrid complexes. European Journal of Medicinal Chemistry. 206: 112694. PMID 32861176 DOI: 10.1016/J.Ejmech.2020.112694  0.342
2020 Probst A, Chisanga K, Dziwornu GA, Haeberli C, Keiser J, Chibale K. Expanding the Activity Profile of Pyrido[1,2-]benzimidazoles: Synthesis and Evaluation of Novel -1-Phenylethanamine Derivatives against . Acs Infectious Diseases. PMID 32786285 DOI: 10.1021/Acsinfecdis.0C00278  0.416
2020 Bryk R, Mundhra S, Jiang X, Wood M, Pfau D, Weber E, Park S, Zhang L, Wilson C, Van der Westhuyzen R, Street L, Chibale K, Zimmerman M, Dartois V, Pastore N, et al. Potentiation of rifampin activity in a mouse model of tuberculosis by activation of host transcription factor EB. Plos Pathogens. 16: e1008567. PMID 32574211 DOI: 10.1371/Journal.Ppat.1008567  0.347
2020 Akester JN, Njaria P, Nchinda AT, Le Manach C, Myrick A, Singh V, Lawrence N, Njoroge M, Taylor D, Moosa A, Smith A, Brooks E, Lenaerts AJ, Robertson GT, Ioerger TR, ... ... Chibale K, et al. Synthesis, Structure Activity Relationship and Mechanistic Studies of Aminoquinazolinones Displaying Antimycobacterial Activity. Acs Infectious Diseases. PMID 32470286 DOI: 10.1021/Acsinfecdis.0C00252  0.437
2020 Van de Walle T, Boone M, Van Puyvelde J, Combrinck J, Smith PJ, Chibale K, Mangelinckx S, D'hooghe M. Synthesis and biological evaluation of novel quinoline-piperidine scaffolds as antiplasmodium agents. European Journal of Medicinal Chemistry. 198: 112330. PMID 32408064 DOI: 10.1016/J.Ejmech.2020.112330  0.453
2020 Singh K, Kaur G, Shanika PS, Dziwornu GA, Okombo J, Chibale K. Structure-activity relationship analyses of fusidic acid derivatives highlight crucial role of the C-21 carboxylic acid moiety to its anti-mycobacterial activity. Bioorganic & Medicinal Chemistry. 115530. PMID 32362386 DOI: 10.1016/J.Bmc.2020.115530  0.375
2020 Vanaerschot M, Murithi JM, Pasaje CFA, Ghidelli-Disse S, Dwomoh L, Bird M, Spottiswoode N, Mittal N, Arendse LB, Owen ES, Wicht KJ, Siciliano G, Bösche M, Yeo T, Kumar TRS, ... ... Chibale K, et al. Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity. Cell Chemical Biology. PMID 32359426 DOI: 10.1016/J.Chembiol.2020.04.001  0.34
2020 Mueller R, Reddy V, Nchinda AT, Mebrahtu F, Taylor D, Lawrence N, Tanner L, Barnabe M, Eyermann CJ, Zou B, Kondreddi RR, Lakshminarayana SB, Rottmann M, Street LJ, Chibale K. Lerisetron Analogues with Antimalarial Properties: Synthesis, Structure-Activity Relationship Studies, and Biological Assessment. Acs Omega. 5: 6967-6982. PMID 32258933 DOI: 10.1021/acsomega.0c00327  0.801
2020 Lowe RA, Taylor D, Chibale K, Nelson A, Marsden SP. Synthesis and evaluation of the performance of a small molecule library based on diverse tropane-related scaffolds. Bioorganic & Medicinal Chemistry. 115442. PMID 32209295 DOI: 10.1016/J.Bmc.2020.115442  0.405
2020 Huszár S, Chibale K, Singh V. The quest for the holy grail: new antitubercular chemical entities, targets and strategies. Drug Discovery Today. PMID 32062007 DOI: 10.1016/J.Drudis.2020.02.003  0.32
2020 Strydom N, Kaur G, Dziwornu GA, Okombo J, Wiesner L, Chibale K. Pharmacokinetics and Organ Distribution of C-3 Alkyl Esters as Potential Antimycobacterial Prodrugs of Fusidic Acid. Acs Infectious Diseases. PMID 32011859 DOI: 10.1021/Acsinfecdis.9B00405  0.31
2020 Sinxadi P, Donini C, Johnstone H, Langdon G, Wiesner L, Allen E, Duparc S, Chalon S, McCarthy JS, Lorch U, Chibale K, Möhrle J, Barnes KI. Safety, tolerability, pharmacokinetics and antimalarial activity of the novel phosphatidylinositol 4-kinase inhibitor MMV390048 in healthy volunteers. Antimicrobial Agents and Chemotherapy. PMID 31932368 DOI: 10.1128/Aac.01896-19  0.341
2020 Cheuka PM, Dziwornu G, Okombo J, Chibale K. Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present). Journal of Medicinal Chemistry. PMID 31913032 DOI: 10.1021/Acs.Jmedchem.9B01622  0.382
2019 Minić A, Van de Walle T, Van Hecke K, Combrinck J, Smith PJ, Chibale K, D'hooghe M. Design and synthesis of novel ferrocene-quinoline conjugates and evaluation of their electrochemical and antiplasmodium properties. European Journal of Medicinal Chemistry. 187: 111963. PMID 31865015 DOI: 10.1016/J.Ejmech.2019.111963  0.453
2019 Murithi JM, Owen ES, Istvan ES, Lee MCS, Ottilie S, Chibale K, Goldberg DE, Winzeler EA, Llinás M, Fidock DA, Vanaerschot M. Combining Stage Specificity and Metabolomic Profiling to Advance Antimalarial Drug Discovery. Cell Chemical Biology. PMID 31813848 DOI: 10.1016/J.Chembiol.2019.11.009  0.365
2019 Kaur H, Singh L, Chibale K, Singh K. Structure elaboration of isoniazid: synthesis, in silico molecular docking and antimycobacterial activity of isoniazid-pyrimidine conjugates. Molecular Diversity. PMID 31691051 DOI: 10.1007/S11030-019-10004-1  0.417
2019 Veale C, Lamming D, Swart T, Chibale K, Hoppe HC. Exploring the Anti-Plasmodial 2-Aminopyridines as Potential Anti-Trypanosomal Agents. Chemmedchem. PMID 31670464 DOI: 10.1002/Cmdc.201900492  0.407
2019 Njoroge M, Kaur G, Espinoza-Moraga M, Wasuna A, Dziwornu GA, Seldon R, Taylor D, Okombo J, Warner DF, Chibale K. Semisynthetic Antimycobacterial C-3 Silicate and C-3/ C-21 Ester Derivatives of Fusidic Acid: Pharmacological Evaluation and Stability Studies in Liver Microsomes, Rat Plasma and Mycobacterium tuberculosis culture. Acs Infectious Diseases. PMID 31309823 DOI: 10.1021/Acsinfecdis.9B00208  0.319
2019 Dziwornu GA, Kamunya S, Ntsabo T, Chibale K. Novel antimycobacterial C-21 amide derivatives of the antibiotic fusidic acid: synthesis, pharmacological evaluation and rationalization of media-dependent activity using molecular docking studies in the binding site of human serum albumin. Medchemcomm. 10: 961-969. PMID 31303994 DOI: 10.1039/C9Md00161A  0.375
2019 Baartzes N, Stringer T, Seldon R, Warner DF, Taylor D, Wittlin S, Chibale K, Smith GS. Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights. European Journal of Medicinal Chemistry. 180: 121-133. PMID 31301563 DOI: 10.1016/J.Ejmech.2019.06.069  0.458
2019 Campaniço A, Carrasco MP, Njoroge M, Seldon R, Chibale K, Perdigão J, Portugal I, Warner DF, Moreira R, Lopes F. Azaaurones as potent antimycobacterial agents active against MDR- and XDR-TB. Chemmedchem. PMID 31294529 DOI: 10.1002/Cmdc.201900289  0.39
2019 Attram HD, Wittlin S, Chibale K. Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles. Medchemcomm. 10: 450-455. PMID 31015908 DOI: 10.1039/C8Md00608C  0.4
2019 Noonan TJ, Chibale K, Cheuka PM, Bourne SA, Caira MR. Co-crystal and salt forms of an imidazopyridazine antimalarial drug lead. Journal of Pharmaceutical Sciences. PMID 30817923 DOI: 10.1016/J.Xphs.2019.02.006  0.359
2019 Okombo J, Brunschwig C, Singh K, Dziwornu GA, Barnard L, Njoroge M, Wittlin S, Chibale K. Antimalarial Pyrido[1,2-a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation and Reactive Metabolite Trapping Studies. Acs Infectious Diseases. PMID 30608648 DOI: 10.1021/Acsinfecdis.8B00279  0.409
2019 Noonan TJ, Chibale K, Cheuka PM, Kumar M, Bourne SA, Caira MR. Five Solid Forms of a Potent Imidazopyridazine Antimalarial Drug Lead: A Preformulation Study Crystal Growth & Design. 19: 4683-4697. DOI: 10.1021/Acs.Cgd.9B00575  0.307
2019 Cheuka PM, Mayoka G, Okombo J, Chibale K. Chapter Two - Medicinal chemistry progression of antimalarial hits from phenotypic whole cell screening of SoftFocus libraries Annual Reports in Medicinal Chemistry. 53: 25-71. DOI: 10.1016/Bs.Armc.2019.04.001  0.357
2018 Mayoka G, Keiser J, Haeberli C, Chibale K. Structure-activity relationship and in vitro ADMET studies of N-aryl 3-trifluoromethyl pyrido [1,2-a] benzimidazoles that are efficacious in a mouse model of schistosomiasis. Acs Infectious Diseases. PMID 30580519 DOI: 10.1021/Acsinfecdis.8B00313  0.416
2018 Mayoka G, Njoroge M, Okombo J, Gibhard L, Sanches-Vaz M, Fontinha D, Birkholtz LM, Reader J, van der Watt M, Coetzer TL, Lauterbach S, Churchyard A, Bezuidenhout B, Egan TJ, Yeates CL, ... ... Chibale K, et al. Structure-activity relationship studies and Plasmodium life cycle profiling identifies pan-active N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazoles which are efficacious in an in vivo mouse model of malaria. Journal of Medicinal Chemistry. PMID 30562027 DOI: 10.1021/Acs.Jmedchem.8B01769  0.424
2018 Kumar M, Okombo J, Mambwe D, Taylor D, Lawrence N, Reader J, Watt MV, Fontinha D, Sanches-Vaz M, C Bezuidenhout B, Lauterbach S, Liebenberg D, Birkholtz LM, Coetzer TL, Prudêncio M, ... ... Chibale K, et al. Multistage Antiplasmodium Activity of Astemizole Analogues and Inhibition of Hemozoin Formation as a Contributor to Their Mode of Action. Acs Infectious Diseases. PMID 30525439 DOI: 10.1021/Acsinfecdis.8B00272  0.447
2018 Cheuka PM, Lawrence N, Taylor D, Wittlin S, Chibale K. Antiplasmodial imidazopyridazines: structure-activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles. Medchemcomm. 9: 1733-1745. PMID 30429978 DOI: 10.1039/C8Md00382C  0.429
2018 Rylands LI, Welsh A, Maepa K, Stringer T, Taylor D, Chibale K, Smith GS. Structure-activity relationship studies of antiplasmodial cyclometallated ruthenium(II), rhodium(III) and iridium(III) complexes of 2-phenylbenzimidazoles. European Journal of Medicinal Chemistry. 161: 11-21. PMID 30342422 DOI: 10.1016/J.Ejmech.2018.10.019  0.38
2018 Le Manach C, Paquet T, Wicht KJ, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, ... Chibale K, et al. Anti-malarial lead optimization studies on a 2,6-imidazopyridine series within a constrained chemical space to circumvent atypical dose-response curves against multi-drug resistant parasite strains. Journal of Medicinal Chemistry. PMID 30256636 DOI: 10.1021/Acs.Jmedchem.8B01333  0.414
2018 Gibhard L, Njoroge M, Paquet T, Brunschwig C, Taylor D, Lawrence N, Abay E, Wittlin S, Wiesner L, Street LJ, Chibale K, Basarab GS. Investigating sulfoxide to sulfone conversion as a prodrug strategy for a PI4K inhibitor in a humanized mouse model of malaria. Antimicrobial Agents and Chemotherapy. PMID 30249687 DOI: 10.1128/Aac.00261-18  0.349
2018 Okombo J, Chibale K. Recent updates in the discovery and development of novel antimalarial drug candidates. Medchemcomm. 9: 437-453. PMID 30108934 DOI: 10.1039/C7Md00637C  0.343
2018 Kaur G, Pavadai E, Wittlin S, Chibale K. 3D-QSAR Modeling and Synthesis of New Fusidic Acid Derivatives as Antiplasmodial Agents. Journal of Chemical Information and Modeling. PMID 30040885 DOI: 10.1021/Acs.Jcim.8B00105  0.454
2018 Kaur G, Pavadai E, Wittlin S, Chibale K. 3D-QSAR Modeling and Synthesis of New Fusidic Acid Derivatives as Antiplasmodial Agents. Journal of Chemical Information and Modeling. PMID 30040885 DOI: 10.1021/acs.jcim.8b00105  0.348
2018 Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, ... ... Chibale K, et al. UCT943, a next generation PI4K inhibitor preclinical candidate for the treatment of malaria. Antimicrobial Agents and Chemotherapy. PMID 29941635 DOI: 10.1128/Aac.00012-18  0.399
2018 Kandepedu N, Gonzalez Cabrera D, Eedubilli S, Taylor D, Brunschwig C, Gibhard L, Njoroge M, Lawrence N, Paquet T, Eyermann CJ, Spangenberg T, Basarab GS, Street LJ, Chibale K. Identification, Characterization and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria. Journal of Medicinal Chemistry. PMID 29889526 DOI: 10.1021/Acs.Jmedchem.8B00648  0.437
2018 Gonzalez Cabrera D, Horatscheck A, Wilson CR, Basarab GS, Eyermann CJ, Chibale K. Plasmodial kinase inhibitors - License to cure? Journal of Medicinal Chemistry. PMID 29771541 DOI: 10.1021/Acs.Jmedchem.8B00329  0.351
2018 Martinez-Grau MA, Valcarcel ICG, Early JV, Gessner RK, de Melo CS, de la Nava EMM, Korkegian A, Ovechkina Y, Flint L, Gravelle A, Cramer JW, Desai PV, Street LJ, Odingo J, Masquelin T, ... Chibale K, et al. Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis. Bioorganic & Medicinal Chemistry Letters. PMID 29680666 DOI: 10.1016/J.Bmcl.2018.04.028  0.442
2018 Nchinda AT, Le Manach C, Paquet T, Gonzalez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jimenez-Diaz MB, Martínez-Martínez MS, Ferrer S, Angulo-Barturen I, ... ... Chibale K, et al. Identification of fast-acting 2,6-disubstituted imidazopyridines that are efficacious in the in vivo humanized Plasmodium falciparum NODscidIL2Rγnull mouse model of malaria. Journal of Medicinal Chemistry. PMID 29665687 DOI: 10.1021/Acs.Jmedchem.8B00382  0.383
2018 Murugesan D, Ray PC, Bayliss T, Prosser GA, Harrison JR, Green K, Soares de Melo C, Feng TS, Street LJ, Chibale K, Warner DF, Mizrahi V, Epemolu O, Scullion P, Ellis L, et al. 2-Mercapto-quinazolinones as inhibitors of NDH-2 and Mycobacterium tuberculosis: Structure-activity relationships, mechanism of action and ADME characterization. Acs Infectious Diseases. PMID 29522317 DOI: 10.1021/Acsinfecdis.7B00275  0.39
2018 Chopra R, Chibale K, Singh K. Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity. European Journal of Medicinal Chemistry. 148: 39-53. PMID 29454189 DOI: 10.1016/J.Ejmech.2018.02.021  0.389
2018 van der Watt ME, Reader J, Churchyard A, Nondaba SH, Lauterbach SB, Niemand J, Abayomi S, van Biljon RA, Connacher JI, van Wyk RDJ, Le Manach C, Paquet T, González Cabrera D, Brunschwig C, Theron A, ... ... Chibale K, et al. Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials. The Journal of Antimicrobial Chemotherapy. PMID 29420756 DOI: 10.1093/Jac/Dky008  0.41
2017 Pavadai E, Kaur G, Wittlin S, Chibale K. Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening. Medchemcomm. 8: 1152-1157. PMID 30108825 DOI: 10.1039/C7Md00063D  0.436
2017 Kumar M, Singh K, Ngwane AH, Hamzabegovic F, Abate G, Baker B, Wiid I, Hoft DF, Ruminski P, Chibale K. Reversed isoniazids: Design, synthesis and evaluation against Mycobacterium tuberculosis. Bioorganic & Medicinal Chemistry. PMID 29373270 DOI: 10.1016/J.Bmc.2017.12.047  0.413
2017 Fienberg S, Cozier GE, Acharya KR, Chibale K, Sturrock ED. The Design and Development of a Potent and Selective Novel Diprolyl Derivative That Binds to the N-Domain of Angiotensin-I Converting Enzyme. Journal of Medicinal Chemistry. PMID 29206036 DOI: 10.1021/Acs.Jmedchem.7B01478  0.329
2017 Joshi MC, Okombo J, Nsumiwa S, Ndove J, Taylor D, Wiesner L, Hunter R, Chibale K, Egan TJ. 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice. Journal of Medicinal Chemistry. 60: 10245-10256. PMID 29185748 DOI: 10.1021/Acs.Jmedchem.7B01537  0.428
2017 Wilson CR, Gessner RK, Moosa A, Seldon R, Warner DF, Mizrahi V, Soares de Melo C, Simelane SB, Nchinda AT, Abay E, Taylor D, Njoroge M, Brunschwig C, Lawrence N, Boshoff HIM, ... ... Chibale K, et al. Novel Anti-tubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure Activity Relationship and Target Identification Studies. Journal of Medicinal Chemistry. PMID 29148755 DOI: 10.1021/Acs.Jmedchem.7B01347  0.445
2017 Stringer T, Seldon R, Liu N, Warner DF, Tam C, Cheng LW, Land KM, Smith PJ, Chibale K, Smith GS. Antimicrobial activity of organometallic isonicotinyl and pyrazinyl ferrocenyl-derived complexes. Dalton Transactions (Cambridge, England : 2003). PMID 28713884 DOI: 10.1039/C7Dt01952A  0.39
2017 Okombo J, Chibale K. Insights into Integrated Lead Generation and Target Identification in Malaria and Tuberculosis Drug Discovery. Accounts of Chemical Research. 50: 1606-1616. PMID 28636311 DOI: 10.1021/Acs.Accounts.6B00631  0.396
2017 Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, ... ... Chibale K, et al. Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase. Science Translational Medicine. 9. PMID 28446690 DOI: 10.1126/Scitranslmed.Aad9735  0.384
2017 Okombo J, Singh K, Mayoka G, Ndubi F, Barnard L, Njogu PM, Njoroge M, Gibhard L, Brunschwig C, Vargas M, Keiser J, Egan TJ, Chibale K. Antischistosomal Activity of Pyrido[1,2-a]benzimidazole Derivatives and Correlation with Inhibition of β-haematin Formation. Acs Infectious Diseases. PMID 28440625 DOI: 10.1021/Acsinfecdis.6B00205  0.423
2017 Vreese R, Kock C, Smith PJ, Chibale K, D'hooghe M. Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents. Future Medicinal Chemistry. PMID 28263085 DOI: 10.4155/Fmc-2016-0215  0.34
2017 Mutai P, Breuzard G, Pagano A, Allegro D, Peyrot V, Chibale K. Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents. Bioorganic & Medicinal Chemistry. 25: 1652-1665. PMID 28174064 DOI: 10.1016/J.Bmc.2017.01.035  0.397
2017 Singh K, Okombo J, Brunschwig C, Ndubi F, Barnard L, Wilkinson C, Njogu PM, Njoroge M, Laing L, Machado M, Prudêncio M, Reader J, Botha ME, Nondaba SH, Birkholtz LM, ... ... Chibale K, et al. Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics and In Vivo Oral Efficacy in a Mouse Model. Journal of Medicinal Chemistry. PMID 28094524 DOI: 10.1021/Acs.Jmedchem.6B01641  0.383
2016 Cheuka PM, Mayoka G, Mutai P, Chibale K. The Role of Natural Products in Drug Discovery and Development against Neglected Tropical Diseases. Molecules (Basel, Switzerland). 22. PMID 28042865 DOI: 10.3390/Molecules22010058  0.313
2016 Espinoza-Moraga M, Singh K, Njoroge M, Kaur G, Okombo J, De Kock C, Smith PJ, Wittlin S, Chibale K. Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents. Bioorganic & Medicinal Chemistry Letters. PMID 28012840 DOI: 10.1016/J.Bmcl.2016.11.077  0.374
2016 Adams M, Stringer T, de Kock C, Smith PJ, Land KM, Liu N, Tam C, Cheng LW, Njoroge M, Chibale K, Smith GS. Bioisosteric ferrocenyl-containing quinolines with antiplasmodial and antitrichomonal properties. Dalton Transactions (Cambridge, England : 2003). PMID 27858010 DOI: 10.1039/C6Dt03175G  0.441
2016 Le Manach C, Nchinda AT, Paquet T, Gonzalez Cabrera D, Younis Adam Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, ... ... Chibale K, et al. Identification of a potential anti-malarial drug candidate from a series of 2-aminopyrazines by optimization of aqueous solubility and potency across the parasite life-cycle. Journal of Medicinal Chemistry. PMID 27748596 DOI: 10.1021/Acs.Jmedchem.6B01265  0.383
2016 Kumar M, Singh K, Naran K, Hamzabegovic F, Hoft DF, Warner DF, Ruminski P, Abate G, Chibale K. Design, Synthesis, and Evaluation of Novel Hybrid Efflux Pump Inhibitors for Use against Mycobacterium tuberculosis. Acs Infectious Diseases. 2: 714-725. PMID 27737555 DOI: 10.1021/Acsinfecdis.6B00111  0.402
2016 Njogu PM, Guantai EM, Pavadai E, Chibale K. Computer-Aided Drug Discovery Approaches against the Tropical Infectious Diseases Malaria, Tuberculosis, Trypanosomiasis, and Leishmaniasis. Acs Infectious Diseases. 2: 8-31. PMID 27622945 DOI: 10.1021/Acsinfecdis.5B00093  0.305
2016 Ngwane AH, Panayides JL, Chouteau F, Macingwana L, Viljoen A, Baker B, Madikane E, de Kock C, Wiesner L, Chibale K, Parkinson CJ, Mmutlane EM, van Helden P, Wiid I. Design, synthesis, and In vitro antituberculosis activity of 2(5H)-Furanone derivatives. Iubmb Life. PMID 27346745 DOI: 10.1002/Iub.1526  0.449
2016 Pavadai E, El Mazouni F, Wittlin S, de Kock C, Phillips MA, Chibale K. Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening. Journal of Chemical Information and Modeling. 56: 548-62. PMID 26915022 DOI: 10.1021/Acs.Jcim.5B00680  0.424
2016 Adams M, Barnard L, de Kock C, Smith PJ, Wiesner L, Chibale K, Smith GS. Cyclopalladated organosilane-tethered thiosemicarbazones: novel strategies for improving antiplasmodial activity. Dalton Transactions (Cambridge, England : 2003). PMID 26911403 DOI: 10.1039/C5Dt04918K  0.434
2016 Umehara K, Zollinger M, Kigondu E, Witschi M, Juif C, Huth F, Schiller H, Chibale K, Camenisch G. Esterase phenotyping in human liver in vitro: specificity of carboxylesterase inhibitors. Xenobiotica; the Fate of Foreign Compounds in Biological Systems. 46: 862-7. PMID 26887925 DOI: 10.3109/00498254.2015.1133867  0.357
2016 Okombo J, Chibale K. Antiplasmodial drug targets: a patent review (2000 - 2013). Expert Opinion On Therapeutic Patents. 26: 107-30. PMID 26566576 DOI: 10.1517/13543776.2016.1113258  0.374
2016 Blackie MAL, Feng TS, Smith PJ, Chibale K. Synthesis of novel β-lactams and in vitro evaluation against the human malaria parasite Plasmodium falciparum Arkivoc. 2016: 214-235. DOI: 10.3998/Ark.5550190.P009.465  0.45
2016 Pavadai E, El Mazouni F, Wittlin S, De Kock C, Phillips MA, Chibale K. Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening Journal of Chemical Information and Modeling. 56: 548-562. DOI: 10.1021/acs.jcim.5b00680  0.311
2016 Soares de Melo C, Feng T, van der Westhuyzen R, Gessner RK, Street LJ, Morgans GL, Warner DF, Moosa A, Naran K, Lawrence N, Boshoff HI, Barry CE, Harris CJ, Gordon R, Chibale K. Corrigendum to “Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization” [Bioorg. Med. Chem. 23 (2015) 7240–7250] Bioorganic & Medicinal Chemistry. 24: 314. DOI: 10.1016/J.Bmc.2015.12.015  0.328
2016 Adams M, de Kock C, Smith PJ, Chibale K, Smith GS. Evaluation of Ferrocenyl-Containing Benzothiazoles as Potential Antiplasmodial Agents European Journal of Inorganic Chemistry. 2017: 242-246. DOI: 10.1002/Ejic.201601000  0.428
2015 Dambuza NS, Smith P, Evans A, Norman J, Taylor D, Andayi A, Egan T, Chibale K, Wiesner L. Antiplasmodial activity, in vivo pharmacokinetics and anti-malarial efficacy evaluation of hydroxypyridinone hybrids in a mouse model. Malaria Journal. 14: 505. PMID 26671222 DOI: 10.1186/S12936-015-1032-5  0.347
2015 van der Westhuyzen R, Winks S, Wilson CR, Boyle GA, Gessner RK, Soares de Melo C, Taylor D, de Kock C, Njoroge M, Brunschwig C, Lawrence N, Rao SP, Sirgel F, van Helden P, Seldon R, ... ... Chibale K, et al. Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A novel anti-mycobacterial class targeting mycobacterial respiration. Journal of Medicinal Chemistry. PMID 26551248 DOI: 10.1021/Acs.Jmedchem.5B01542  0.438
2015 Candice Sde M, Feng TS, van der Westhuyzen R, Gessner RK, Street LJ, Morgans GL, Warner DF, Moosa A, Naran K, Lawrence N, Boshoff HI, Barry CE, Harris CJ, Gordon R, Chibale K. Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization. Bioorganic & Medicinal Chemistry. 23: 7240-50. PMID 26522089 DOI: 10.1016/J.Bmc.2015.10.021  0.428
2015 Le Manach C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, ... ... Chibale K, et al. A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines. Journal of Medicinal Chemistry. 58: 8713-22. PMID 26502160 DOI: 10.1021/Acs.Jmedchem.5B01605  0.414
2015 Thelingwani R, Leandersson C, Bonn B, Smith P, Chibale K, Masimirembwa C. Characterisation of artemisinin-chloroquinoline hybrids for potential metabolic liabilities. Xenobiotica; the Fate of Foreign Compounds in Biological Systems. 1-7. PMID 26338168 DOI: 10.3109/00498254.2015.1070975  0.328
2015 Gonzàlez Cabrera D, Douelle F, Le Manach C, Han Z, Paquet T, Taylor D, Njoroge M, Lawrence N, Wiesner L, Waterson D, Witty MJ, Wittlin S, Street LJ, Chibale K. Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines. Journal of Medicinal Chemistry. 58: 7572-9. PMID 26322748 DOI: 10.1021/Acs.Jmedchem.5B01156  0.368
2015 Ongarora DS, Strydom N, Wicht K, Njoroge M, Wiesner L, Egan TJ, Wittlin S, Jurva U, Masimirembwa CM, Chibale K. Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. Bioorganic & Medicinal Chemistry. 23: 5419-32. PMID 26264839 DOI: 10.1016/J.Bmc.2015.07.051  0.458
2015 Kaur H, Balzarini J, de Kock C, Smith PJ, Chibale K, Singh K. Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. European Journal of Medicinal Chemistry. 101: 52-62. PMID 26114811 DOI: 10.1016/J.Ejmech.2015.06.024  0.379
2015 Chopra R, de Kock C, Smith P, Chibale K, Singh K. Ferrocene-pyrimidine conjugates: Synthesis, electrochemistry, physicochemical properties and antiplasmodial activities. European Journal of Medicinal Chemistry. 100: 1-9. PMID 26057222 DOI: 10.1016/J.Ejmech.2015.05.043  0.403
2015 Njaria PM, Okombo J, Njuguna NM, Chibale K. Chloroquine-containing compounds: a patent review (2010 - 2014). Expert Opinion On Therapeutic Patents. 25: 1003-24. PMID 26013494 DOI: 10.1517/13543776.2015.1050791  0.373
2015 Mutai P, Pavadai E, Wiid I, Ngwane A, Baker B, Chibale K. Synthesis, antimycobacterial evaluation and pharmacophore modeling of analogues of the natural product formononetin. Bioorganic & Medicinal Chemistry Letters. 25: 2510-3. PMID 25977095 DOI: 10.1016/J.Bmcl.2015.04.064  0.374
2015 Dambuza N, Smith P, Evans A, Taylor D, Chibale K, Wiesner L. A Pharmacokinetic Study of Antimalarial 3,5-Diaryl-2-aminopyridine Derivatives. Malaria Research and Treatment. 2015: 405962. PMID 25893131 DOI: 10.1155/2015/405962  0.398
2015 Adams M, de Kock C, Smith PJ, Land KM, Liu N, Hopper M, Hsiao A, Burgoyne AR, Stringer T, Meyer M, Wiesner L, Chibale K, Smith GS. Improved antiparasitic activity by incorporation of organosilane entities into half-sandwich ruthenium(II) and rhodium(III) thiosemicarbazone complexes. Dalton Transactions (Cambridge, England : 2003). 44: 2456-68. PMID 25559246 DOI: 10.1039/C4Dt03234A  0.373
2015 Vandekerckhove S, Van Herreweghe S, Willems J, Danneels B, Desmet T, de Kock C, Smith PJ, Chibale K, D'hooghe M. Synthesis of functionalized 3-, 5-, 6- and 8-aminoquinolines via intermediate (3-pyrrolin-1-yl)- and (2-oxopyrrolidin-1-yl)quinolines and evaluation of their antiplasmodial and antifungal activity. European Journal of Medicinal Chemistry. 92: 91-102. PMID 25544689 DOI: 10.1016/J.Ejmech.2014.12.020  0.463
2015 Sharma RK, Younis Y, Mugumbate G, Njoroge M, Gut J, Rosenthal PJ, Chibale K. Synthesis and structure-activity-relationship studies of thiazolidinediones as antiplasmodial inhibitors of the Plasmodium falciparum cysteine protease falcipain-2. European Journal of Medicinal Chemistry. 90: 507-18. PMID 25486422 DOI: 10.1016/J.Ejmech.2014.11.061  0.447
2015 Kaur G, Singh K, Pavadai E, Njoroge M, Espinoza-Moraga M, De Kock C, Smith PJ, Wittlin S, Chibale K. Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G Medchemcomm. 6: 2023-2028. DOI: 10.1039/C5Md00343A  0.337
2014 Cheuka PM, Cabrera DG, Paquet T, Chibale K. Structure-activity relationship studies of antiplasmodial aminomethylthiazoles. Bioorganic & Medicinal Chemistry Letters. 24: 5207-11. PMID 25316314 DOI: 10.1016/J.Bmcl.2014.09.071  0.435
2014 Le Manach C, Paquet T, Gonzàlez Cabrera D, Younis Y, Taylor D, Wiesner L, Lawrence N, Schwager S, Waterson D, Witty MJ, Wittlin S, Street LJ, Chibale K. Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: Part 2 Journal of Medicinal Chemistry. 57: 8839-8848. PMID 25313449 DOI: 10.1021/Jm500887K  0.434
2014 Thelingwani R, Bonn B, Chibale K, Masimirembwa C. Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity. Expert Opinion On Drug Metabolism & Toxicology. 10: 1313-24. PMID 25219629 DOI: 10.1517/17425255.2014.954547  0.358
2014 Kigondu EM, Wasuna A, Warner DF, Chibale K. Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery. Bioorganic & Medicinal Chemistry. 22: 4453-61. PMID 24997576 DOI: 10.1016/J.Bmc.2014.06.012  0.372
2014 Andayi WA, Egan TJ, Chibale K. Kojic acid derived hydroxypyridinone-chloroquine hybrids: Synthesis, crystal structure, antiplasmodial activity and β-haematin inhibition Bioorganic and Medicinal Chemistry Letters. 24: 3263-3267. PMID 24974345 DOI: 10.1016/J.Bmcl.2014.06.012  0.42
2014 Singh K, Kumar M, Pavadai E, Naran K, Warner DF, Ruminski PG, Chibale K. Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c. Bioorganic & Medicinal Chemistry Letters. 24: 2985-90. PMID 24894561 DOI: 10.1016/J.Bmcl.2014.05.022  0.344
2014 Le Manach C, Gonzàlez Cabrera D, Douelle F, Nchinda AT, Younis Y, Taylor D, Wiesner L, White KL, Ryan E, March C, Duffy S, Avery VM, Waterson D, Witty MJ, Wittlin S, ... ... Chibale K, et al. Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1. Journal of Medicinal Chemistry. 57: 2789-98. PMID 24568587 DOI: 10.1021/Jm500098S  0.407
2014 Abay ET, van der Westhuizen JH, Swart KJ, Gibhard L, Tukulula M, Chibale K, Wiesner L. The development and validation of an LC-MS/MS method for the determination of a new anti-malarial compound (TK900D) in human whole blood and its application to pharmacokinetic studies in mice. Malaria Journal. 13: 42. PMID 24484513 DOI: 10.1186/1475-2875-13-42  0.415
2014 Vandekerckhove S, Desmet T, Tran HG, de Kock C, Smith PJ, Chibale K, D'hooghe M. Synthesis of halogenated 4-quinolones and evaluation of their antiplasmodial activity. Bioorganic & Medicinal Chemistry Letters. 24: 1214-7. PMID 24468411 DOI: 10.1016/J.Bmcl.2013.12.067  0.432
2014 González Cabrera D, Le Manach C, Douelle F, Younis Y, Feng TS, Paquet T, Nchinda AT, Street LJ, Taylor D, de Kock C, Wiesner L, Duffy S, White KL, Zabiulla KM, Sambandan Y, ... ... Chibale K, et al. 2,4-Diaminothienopyrimidines as orally active antimalarial agents. Journal of Medicinal Chemistry. 57: 1014-22. PMID 24446664 DOI: 10.1021/Jm401760C  0.405
2014 Mjambili F, Njoroge M, Naran K, De Kock C, Smith PJ, Mizrahi V, Warner D, Chibale K. Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents. Bioorganic & Medicinal Chemistry Letters. 24: 560-4. PMID 24373723 DOI: 10.1016/J.Bmcl.2013.12.022  0.43
2014 Singh K, Kaur H, Smith P, de Kock C, Chibale K, Balzarini J. Quinoline-pyrimidine hybrids: synthesis, antiplasmodial activity, SAR, and mode of action studies. Journal of Medicinal Chemistry. 57: 435-48. PMID 24354322 DOI: 10.1021/Jm4014778  0.399
2014 Chellan P, Land KM, Shokar A, Au A, An SH, Taylor D, Smith PJ, Riedel T, Dyson PJ, Chibale K, Smith GS. Synthesis and evaluation of new polynuclear organometallic Ru(II), Rh(III) and Ir(III) pyridyl ester complexes as in vitro antiparasitic and antitumor agents. Dalton Transactions (Cambridge, England : 2003). 43: 513-26. PMID 24121555 DOI: 10.1039/C3Dt52090K  0.35
2014 Ghidelli-Disse S, Lafuente-Monasterio MJ, Waterson D, Witty M, Younis Y, Paquet T, Street LJ, Chibale K, Gamo-Benito FJ, Bantscheff M, Drewes G. Identification of Plasmodium PI4 kinase as target of MMV390048 by chemoproteomics Malaria Journal. 13. DOI: 10.1186/1475-2875-13-S1-P38  0.383
2014 Mahajan A, Hans R, Chibale K, Kumar V. Synthesis and medicinal chemistry of selected antitubercular natural products and natural product derivatives Rsc Advances. 4: 15180. DOI: 10.1039/C3Ra46124F  0.355
2014 Kigondu EM, Njoroge M, Singh K, Njuguna N, Warner DF, Chibale K. Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolites Medchemcomm. 5: 502-506. DOI: 10.1039/C3Md00387F  0.364
2014 Singh K, Kaur G, Mjambili F, Smith PJ, Chibale K. Synthesis of metergoline analogues and their evaluation as antiplasmodial agents Medchemcomm. 5: 165-170. DOI: 10.1039/C3Md00310H  0.458
2014 Cruickshank DL, Younis Y, Njuguna NM, Ongarora DSB, Chibale K, Caira MR. Alternative solid-state forms of a potent antimalarial aminopyridine: X-ray crystallographic, thermal and solubility aspects Crystengcomm. 16: 5781-5792. DOI: 10.1039/C3Ce41798K  0.332
2014 Li Y, De Kock C, Smith PJ, Chibale K, Smith GS. Synthesis and evaluation of a carbosilane congener of ferroquine and its corresponding half-sandwich ruthenium and rhodium complexes for antiplasmodial and β-hematin inhibition activity Organometallics. 33: 4345-4348. DOI: 10.1021/Om500622P  0.397
2013 Andayi WA, Egan TJ, Gut J, Rosenthal PJ, Chibale K. Synthesis, Antiplasmodial Activity, and β-Hematin Inhibition of Hydroxypyridone-Chloroquine Hybrids. Acs Medicinal Chemistry Letters. 4: 642-6. PMID 24900724 DOI: 10.1021/Ml4001084  0.359
2013 Njogu PM, Gut J, Rosenthal PJ, Chibale K. Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine. Acs Medicinal Chemistry Letters. 4: 637-41. PMID 24900723 DOI: 10.1021/Ml400164T  0.388
2013 Tukulula M, Njoroge M, Abay ET, Mugumbate GC, Wiesner L, Taylor D, Gibhard L, Norman J, Swart KJ, Gut J, Rosenthal PJ, Barteau S, Streckfuss J, Kameni-Tcheudji J, Chibale K. Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. Acs Medicinal Chemistry Letters. 4: 1198-202. PMID 24900630 DOI: 10.1021/Ml400311R  0.414
2013 Tukulula M, Sharma RK, Meurillon M, Mahajan A, Naran K, Warner D, Huang J, Mekonnen B, Chibale K. Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives. Acs Medicinal Chemistry Letters. 4: 128-31. PMID 24900574 DOI: 10.1021/Ml300362A  0.429
2013 Vial H, Taramelli D, Boulton IC, Ward SA, Doerig C, Chibale K. CRIMALDDI: platform technologies and novel anti-malarial drug targets. Malaria Journal. 12: 396. PMID 24498961 DOI: 10.1186/1475-2875-12-396  0.361
2013 Hooft van Huijsduijnen R, Guy RK, Chibale K, Haynes RK, Peitz I, Kelter G, Phillips MA, Vennerstrom JL, Yuthavong Y, Wells TN. Anticancer properties of distinct antimalarial drug classes. Plos One. 8: e82962. PMID 24391728 DOI: 10.1371/Journal.Pone.0082962  0.588
2013 Le Manach C, Scheurer C, Sax S, Schleiferböck S, Cabrera DG, Younis Y, Paquet T, Street L, Smith P, Ding XC, Waterson D, Witty MJ, Leroy D, Chibale K, Wittlin S. Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum Malaria Journal. 12. PMID 24237770 DOI: 10.1186/1475-2875-12-424  0.43
2013 Mugumbate G, Newton AS, Rosenthal PJ, Gut J, Moreira R, Chibale K, Guedes RC. Novel anti-plasmodial hits identified by virtual screening of the ZINC database. Journal of Computer-Aided Molecular Design. 27: 859-71. PMID 24158745 DOI: 10.1007/S10822-013-9685-Z  0.424
2013 Younis Y, Douelle F, González Cabrera D, Le Manach C, Nchinda AT, Paquet T, Street LJ, White KL, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Wittlin S, Charman SA, ... Chibale K, et al. Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity. Journal of Medicinal Chemistry. 56: 8860-71. PMID 24099149 DOI: 10.1021/Jm401278D  0.439
2013 Chigorimbo-Murefu NT, Njoroge M, Louw S, Mugumbate G, Chibale K. Drug metabolite generation using a laboratory evolved NADPH independent cytochrome P450: application of in vitro and in silico approaches. Drug Metabolism Letters. 7: 68-77. PMID 23957950 DOI: 10.2174/18723128112069990014  0.311
2013 Younis Y, Street LJ, Waterson D, Witty MJ, Chibale K. Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part 2: hits from SoftFocus kinase and other libraries. Journal of Medicinal Chemistry. 56: 7750-4. PMID 23927599 DOI: 10.1021/Jm400279Y  0.328
2013 Tukulula M, Njoroge M, Mugumbate GC, Gut J, Rosenthal PJ, Barteau S, Streckfuss J, Heudi O, Kameni-Tcheudji J, Chibale K. Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents. Bioorganic & Medicinal Chemistry. 21: 4904-13. PMID 23896611 DOI: 10.1016/J.Bmc.2013.06.067  0.423
2013 Singh K, Kaur H, Chibale K, Balzarini J. Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. European Journal of Medicinal Chemistry. 66: 314-23. PMID 23811093 DOI: 10.1016/J.Ejmech.2013.05.046  0.403
2013 Espinoza-Moraga M, Njuguna NM, Mugumbate G, Caballero J, Chibale K. In silico comparison of antimycobacterial natural products with known antituberculosis drugs. Journal of Chemical Information and Modeling. 53: 649-60. PMID 23410241 DOI: 10.1021/Ci300467B  0.364
2013 Njogu PM, Chibale K. Recent developments in rationally designed multitarget antiprotozoan agents. Current Medicinal Chemistry. 20: 1715-42. PMID 23410169 DOI: 10.2174/0929867311320130010  0.302
2013 Adams M, Li Y, Khot H, De Kock C, Smith PJ, Land K, Chibale K, Smith GS. The synthesis and antiparasitic activity of aryl- and ferrocenyl-derived thiosemicarbazone ruthenium(II)-arene complexes. Dalton Transactions (Cambridge, England : 2003). 42: 4677-85. PMID 23361649 DOI: 10.1039/C3Dt32740J  0.313
2013 D'hooghe M, Vervisch K, Törnroos KW, Verhaeghe T, Desmet T, Lategan C, Smith PJ, Chibale K, De Kimpe N. Synthesis of 2-aminomethyl-4-phenyl-1-azabicyclo[2.2.1]heptanes via LiAlH₄-induced reductive cyclization of 2-(4-chloro-2-cyano-2-phenylbutyl)aziridines and evaluation of their antimalarial activity. Bioorganic & Medicinal Chemistry Letters. 23: 1507-10. PMID 23347684 DOI: 10.1016/J.Bmcl.2012.12.029  0.362
2013 Vandekerckhove S, Müller C, Vogt D, Lategan C, Smith PJ, Chibale K, De Kimpe N, D'hooghe M. Synthesis and antiplasmodial evaluation of novel (4-aminobutyloxy)quinolines. Bioorganic & Medicinal Chemistry Letters. 23: 318-22. PMID 23195733 DOI: 10.1016/J.Bmcl.2012.10.094  0.446
2013 Vandekerckhove S, De Moor S, Segers D, de Kock C, Smith PJ, Chibale K, De Kimpe N, D'hooghe M. Synthesis and antiplasmodial evaluation of aziridine–(iso)quinoline hybrids and their ring-opening products Medchemcomm. 4: 724. DOI: 10.1039/C3Md20377H  0.43
2013 Chellan P, Land KM, Shokar A, Au A, An SH, Taylor D, Smith PJ, Chibale K, Smith GS. Di- and Trinuclear Ruthenium-, Rhodium-, and Iridium-Functionalized Pyridyl Aromatic Ethers: A New Class of Antiparasitic Agents Organometallics. 32: 4793-4804. DOI: 10.1021/Om400493K  0.373
2013 Mutai P, Heydenreich M, Thoithi G, Mugumbate G, Chibale K, Yenesew A. 3-Hydroxyisoflavanones from the stem bark of Dalbergia melanoxylon: Isolation, antimycobacterial evaluation and molecular docking studies Phytochemistry Letters. 6: 671-675. DOI: 10.1016/J.Phytol.2013.08.018  0.357
2013 Adams M, de Kock C, Smith PJ, Malatji P, Hutton AT, Chibale K, Smith GS. Heterobimetallic ferrocenylthiosemicarbazone palladium(II) complexes: Synthesis, electrochemistry and antiplasmodial evaluation Journal of Organometallic Chemistry. 739: 15-20. DOI: 10.1016/J.Jorganchem.2013.04.017  0.334
2013 Adams M, de Kock C, Smith PJ, Chibale K, Smith GS. Synthesis, characterization and antiplasmodial evaluation of cyclopalladated thiosemicarbazone complexes Journal of Organometallic Chemistry. 736: 19-26. DOI: 10.1016/J.Jorganchem.2013.02.024  0.303
2012 Chigorimbo-Murefu NT, Njoroge M, Nzila A, Louw S, Masimirembwa C, Chibale K. Biotransformation and biocatalysis: roles and applications in the discovery of antimalarials. Future Medicinal Chemistry. 4: 2325-36. PMID 23234554 DOI: 10.4155/Fmc.12.173  0.335
2012 Paquet T, Gordon R, Waterson D, Witty MJ, Chibale K. Antimalarial aminothiazoles and aminopyridines from phenotypic whole-cell screening of a SoftFocus(®) library. Future Medicinal Chemistry. 4: 2265-77. PMID 23234550 DOI: 10.4155/Fmc.12.176  0.385
2012 González Cabrera D, Douelle F, Younis Y, Feng TS, Le Manach C, Nchinda AT, Street LJ, Scheurer C, Kamber J, White KL, Montagnat OD, Ryan E, Katneni K, Zabiulla KM, Joseph JT, ... ... Chibale K, et al. Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines. Journal of Medicinal Chemistry. 55: 11022-30. PMID 23189922 DOI: 10.1021/Jm301476B  0.467
2012 Tukulula M, Little S, Gut J, Rosenthal PJ, Wan B, Franzblau SG, Chibale K. The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives. European Journal of Medicinal Chemistry. 57: 259-67. PMID 23064162 DOI: 10.1016/J.Ejmech.2012.08.047  0.44
2012 Njuguna NM, Ongarora DS, Chibale K. Artemisinin derivatives: a patent review (2006 - present). Expert Opinion On Therapeutic Patents. 22: 1179-203. PMID 22971128 DOI: 10.1517/13543776.2012.724063  0.339
2012 Aminake MN, Mahajan A, Kumar V, Hans R, Wiesner L, Taylor D, de Kock C, Grobler A, Smith PJ, Kirschner M, Rethwilm A, Pradel G, Chibale K. Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. Bioorganic & Medicinal Chemistry. 20: 5277-89. PMID 22858300 DOI: 10.1016/J.Bmc.2012.06.038  0.362
2012 Ongarora DS, Gut J, Rosenthal PJ, Masimirembwa CM, Chibale K. Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: synthesis and pharmacological evaluation. Bioorganic & Medicinal Chemistry Letters. 22: 5046-50. PMID 22749280 DOI: 10.1016/J.Bmcl.2012.06.010  0.408
2012 Thelingwani RS, Dhansay K, Smith P, Chibale K, Masimirembwa CM. Potent inhibition of CYP1A2 by Frutinone A, an active ingredient of the broad spectrum antimicrobial herbal extract from P. fruticosa. Xenobiotica; the Fate of Foreign Compounds in Biological Systems. 42: 989-1000. PMID 22533317 DOI: 10.3109/00498254.2012.681077  0.358
2012 Singh K, Kaur H, Chibale K, Balzarini J, Little S, Bharatam PV. 2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies. European Journal of Medicinal Chemistry. 52: 82-97. PMID 22459876 DOI: 10.1016/J.Ejmech.2012.03.007  0.435
2012 Geary TG, Chibale K, Abegaz B, Andrae-Marobela K, Ubalijoro E. A new approach for anthelmintic discovery for humans. Trends in Parasitology. 28: 176-181. PMID 22424638 DOI: 10.1016/J.Pt.2012.02.006  0.322
2012 Younis Y, Douelle F, Feng TS, González Cabrera D, Le Manach C, Nchinda AT, Duffy S, White KL, Shackleford DM, Morizzi J, Mannila J, Katneni K, Bhamidipati R, Zabiulla KM, Joseph JT, ... ... Chibale K, et al. 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. Journal of Medicinal Chemistry. 55: 3479-87. PMID 22390538 DOI: 10.1021/Jm3001373  0.405
2012 Njuguna NM, Masimirembwa C, Chibale K. Identification and characterization of reactive metabolites in natural products-driven drug discovery. Journal of Natural Products. 75: 507-13. PMID 22296642 DOI: 10.1021/Np200786J  0.326
2012 Kobarfard F, Yardley V, Little S, Daryaee F, Chibale K. Synthesis of aminoquinoline-based aminoalcohols and oxazolidinones and their antiplasmodial activity. Chemical Biology & Drug Design. 79: 326-31. PMID 22129095 DOI: 10.1111/J.1747-0285.2011.01278.X  0.386
2012 Li Y, de Kock C, Smith PJ, Guzgay H, Hendricks DT, Naran K, Mizrahi V, Warner DF, Chibale K, Smith GS. Synthesis, Characterization, and Pharmacological Evaluation of Silicon-Containing Aminoquinoline Organometallic Complexes As Antiplasmodial, Antitumor, and Antimycobacterial Agents Organometallics. 32: 141-150. DOI: 10.1021/Om300945C  0.384
2011 D'hooghe M, Vandekerckhove S, Mollet K, Vervisch K, Dekeukeleire S, Lehoucq L, Lategan C, Smith PJ, Chibale K, De Kimpe N. Synthesis of 2-amino-3-arylpropan-1-ols and 1-(2,3-diaminopropyl)-1,2,3-triazoles and evaluation of their antimalarial activity. Beilstein Journal of Organic Chemistry. 7: 1745-52. PMID 22238554 DOI: 10.3762/Bjoc.7.205  0.439
2011 Tacon C, Guantai EM, Smith PJ, Chibale K. Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents. Bioorganic & Medicinal Chemistry. 20: 893-902. PMID 22196513 DOI: 10.1016/J.Bmc.2011.11.060  0.348
2011 González Cabrera D, Douelle F, Feng TS, Nchinda AT, Younis Y, White KL, Wu Q, Ryan E, Burrows JN, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K. Novel orally active antimalarial thiazoles. Journal of Medicinal Chemistry. 54: 7713-9. PMID 21966980 DOI: 10.1021/Jm201108K  0.401
2011 Nzila A, Ma Z, Chibale K. Drug repositioning in the treatment of malaria and TB. Future Medicinal Chemistry. 3: 1413-1426. PMID 21879845 DOI: 10.4155/Fmc.11.95  0.343
2011 Zishiri VK, Joshi MC, Hunter R, Chibale K, Smith PJ, Summers RL, Martin RE, Egan TJ. Quinoline antimalarials containing a dibemethin group are active against chloroquinone-resistant Plasmodium falciparum and inhibit chloroquine transport via the P. falciparum chloroquine-resistance transporter (PfCRT). Journal of Medicinal Chemistry. 54: 6956-68. PMID 21875063 DOI: 10.1021/Jm2009698  0.42
2011 Singh P, Sachdeva S, Raj R, Kumar V, Mahajan MP, Nasser S, Vivas L, Gut J, Rosenthal PJ, Feng TS, Chibale K. Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives. Bioorganic & Medicinal Chemistry Letters. 21: 4561-3. PMID 21705220 DOI: 10.1016/J.Bmcl.2011.05.119  0.376
2011 Ndakala AJ, Gessner RK, Gitari PW, October N, White KL, Hudson A, Fakorede F, Shackleford DM, Kaiser M, Yeates C, Charman SA, Chibale K. Antimalarial pyrido[1,2-a]benzimidazoles. Journal of Medicinal Chemistry. 54: 4581-9. PMID 21644541 DOI: 10.1021/Jm200227R  0.45
2011 Feng TS, Guantai EM, Nell M, Van Rensburg CEJ, Ncokazi K, Egan TJ, Hoppe HC, Chibale K. Effects of highly active novel artemisinin-chloroquinoline hybrid compounds on β-hematin formation, parasite morphology and endocytosis in Plasmodium falciparum Biochemical Pharmacology. 82: 236-247. PMID 21596024 DOI: 10.1016/J.Bcp.2011.04.018  0.451
2011 Mahajan A, Kremer L, Louw S, Guérardel Y, Guéradel Y, Chibale K, Biot C. Synthesis and in vitro antitubercular activity of ferrocene-based hydrazones. Bioorganic & Medicinal Chemistry Letters. 21: 2866-8. PMID 21507641 DOI: 10.1016/J.Bmcl.2011.03.082  0.427
2011 Guantai EM, Ncokazi K, Egan TJ, Gut J, Rosenthal PJ, Bhampidipati R, Kopinathan A, Smith PJ, Chibale K. Enone- and chalcone-chloroquinoline hybrid analogues: In silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies Journal of Medicinal Chemistry. 54: 3637-3649. PMID 21500839 DOI: 10.1021/Jm200149E  0.384
2011 Feng TS, Guantai EM, Nell MJ, Van Rensburg CEJ, Hoppe HC, Chibale K. Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction Bioorganic and Medicinal Chemistry Letters. 21: 2882-2886. PMID 21489789 DOI: 10.1016/J.Bmcl.2011.03.090  0.406
2011 Singh K, Singh K, Wan B, Franzblau S, Chibale K, Balzarini J. Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity. European Journal of Medicinal Chemistry. 46: 2290-4. PMID 21450375 DOI: 10.1016/J.Ejmech.2011.03.010  0.382
2011 Guantai E, Chibale K. How can natural products serve as a viable source of lead compounds for the development of new/novel anti-malarials? Malaria Journal. S2. PMID 21411013 DOI: 10.1186/1475-2875-10-S1-S2  0.409
2011 Burrows JN, Chibale K, Wells TN. The state of the art in anti-malarial drug discovery and development. Current Topics in Medicinal Chemistry. 11: 1226-54. PMID 21401508 DOI: 10.2174/156802611795429194  0.314
2011 Hans RH, Wiid IJ, van Helden PD, Wan B, Franzblau SG, Gut J, Rosenthal PJ, Chibale K. Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents. Bioorganic & Medicinal Chemistry Letters. 21: 2055-8. PMID 21376591 DOI: 10.1016/J.Bmcl.2011.02.008  0.457
2011 D'hooghe M, Kenis S, Vervisch K, Lategan C, Smith PJ, Chibale K, De Kimpe N. Synthesis of 2-(aminomethyl)aziridines and their microwave-assisted ring opening to 1,2,3-triaminopropanes as novel antimalarial pharmacophores. European Journal of Medicinal Chemistry. 46: 579-87. PMID 21183259 DOI: 10.1016/J.Ejmech.2010.11.037  0.346
2011 Blackie MA, Chibale K. Metallocene antimalarials: the continuing quest. Metal-Based Drugs. 2008: 495123. PMID 18274662 DOI: 10.1155/2008/495123  0.448
2011 Khanye SD, Gut J, Rosenthal PJ, Chibale K, Smith GS. Ferrocenylthiosemicarbazones conjugated to a poly(propyleneimine) dendrimer scaffold: Synthesis and in vitro antimalarial activity Journal of Organometallic Chemistry. 696: 3296-3300. DOI: 10.1016/J.Jorganchem.2011.07.028  0.424
2011 Khanye SD, Wan B, Franzblau SG, Gut J, Rosenthal PJ, Smith GS, Chibale K. Synthesis and in vitro antimalarial and antitubercular activity of gold(III) complexes containing thiosemicarbazone ligands Journal of Organometallic Chemistry. 696: 3392-3396. DOI: 10.1016/J.Jorganchem.2011.07.026  0.383
2010 Guantai EM, Ncokazi K, Egan TJ, Gut J, Rosenthal PJ, Smith PJ, Chibale K. Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds Bioorganic and Medicinal Chemistry. 18: 8243-8256. PMID 21044845 DOI: 10.1016/J.Bmc.2010.10.009  0.43
2010 Hans RH, Su H, Chibale K. Novel tetracyclic structures from the synthesis of thiolactone-isatin hybrids. Beilstein Journal of Organic Chemistry. 6. PMID 20703386 DOI: 10.3762/Bjoc.6.78  0.364
2010 Guantai EM, Chibale K. Chloroquine resistance: proposed mechanisms and countermeasures. Current Drug Delivery. 7: 312-323. PMID 20695842 DOI: 10.2174/156720110793360577  0.302
2010 Khanye SD, Smith GS, Lategan C, Smith PJ, Gut J, Rosenthal PJ, Chibale K. Synthesis and in vitro evaluation of gold(I) thiosemicarbazone complexes for antimalarial activity. Journal of Inorganic Biochemistry. 104: 1079-83. PMID 20621360 DOI: 10.1016/J.Jinorgbio.2010.06.005  0.332
2010 Hans RH, Gut J, Rosenthal PJ, Chibale K. Comparison of the antiplasmodial and falcipain-2 inhibitory activity of beta-amino alcohol thiolactone-chalcone and isatin-chalcone hybrids. Bioorganic & Medicinal Chemistry Letters. 20: 2234-7. PMID 20206517 DOI: 10.1016/J.Bmcl.2010.02.017  0.365
2010 Hans RH, Guantai EM, Lategan C, Smith PJ, Wan B, Franzblau SG, Gut J, Rosenthal PJ, Chibale K. Synthesis, antimalarial and antitubercular activity of acetylenic chalcones. Bioorganic & Medicinal Chemistry Letters. 20: 942-4. PMID 20045640 DOI: 10.1016/J.Bmcl.2009.12.062  0.404
2010 Chellan P, Nasser S, Vivas L, Chibale K, Smith GS. Cyclopalladated complexes containing tridentate thiosemicarbazone ligands of biological significance: Synthesis, structure and antimalarial activity Journal of Organometallic Chemistry. 695: 2225-2232. DOI: 10.1016/J.Jorganchem.2010.06.010  0.323
2010 Chellan P, Shunmoogam-Gounden N, Hendricks DT, Gut J, Rosenthal PJ, Lategan C, Smith PJ, Chibale K, Smith GS. Synthesis, Structure and in Vitro Biological Screening of Palladium(II) Complexes of Functionalised Salicylaldimine Thiosemicarbazones as Antimalarial and Anticancer Agents European Journal of Inorganic Chemistry. 2010: 3520-3528. DOI: 10.1002/Ejic.201000317  0.325
2010 NICOLAOU KC, TRUJILLO JI, CHIBALE K. ChemInform Abstract: Design, Synthesis, and Biological Evaluation of Carbohydrate-Based Mimetics of cRGDFV. Cheminform. 28: no-no. DOI: 10.1002/chin.199743239  0.323
2009 Blackie MA, Yardley V, Chibale K. Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo. Bioorganic & Medicinal Chemistry Letters. 20: 1078-80. PMID 20034790 DOI: 10.1016/J.Bmcl.2009.12.030  0.373
2009 Stevens AT, Caira MR, Bull JR, Chibale K. Cycloaddition and one-carbon homologation studies in the synthesis of advanced iridoid precursors. Organic & Biomolecular Chemistry. 7: 3527-36. PMID 19675910 DOI: 10.1039/B902452B  0.313
2009 D'hooghe M, Dekeukeleire S, Mollet K, Lategan C, Smith PJ, Chibale K, De Kimpe N. Synthesis of novel 2-alkoxy-3-amino-3-arylpropan-1-ols and 5-alkoxy-4-aryl-1,3-oxazinanes with antimalarial activity. Journal of Medicinal Chemistry. 52: 4058-62. PMID 19463002 DOI: 10.1021/Jm9002632  0.431
2009 Kumar V, Mahajan A, Chibale K. Synthetic medicinal chemistry of selected antimalarial natural products. Bioorganic & Medicinal Chemistry. 17: 2236-75. PMID 19157883 DOI: 10.1016/J.Bmc.2008.10.072  0.363
2009 Chibale K, Gessner R. A New and Simple Synthesis of Sulfonyl Ureas from Sulfonamides and N-Alkyl-1,2,4-dithiazolidine-3,5-diones Synlett. 2009: 2839-2843. DOI: 10.1055/S-0029-1217960  0.309
2009 Watermeyer ND, Chibale K, Caira MR. Pharmacologically Relevant Bifunctional Compounds Containing Chloroquinoline and Dihydropyrimidone Moieties: Syntheses and Crystal Structures of a Target Molecule and Selected Intermediates Journal of Chemical Crystallography. 39: 753-760. DOI: 10.1007/S10870-009-9568-2  0.333
2008 Musonda CC, Yardley V, Carvalho De Souza RC, Ncokazi K, Egan TJ, Chibale K. Antiplasmodial, β-haematin inhibition, antitrypanosomal and cytotoxic activity in vitro of novel 4-aminoquinoline 2-imidazolines Organic and Biomolecular Chemistry. 6: 4446-4451. PMID 19005606 DOI: 10.1039/B813007H  0.436
2008 October N, Watermeyer ND, Yardley V, Egan TJ, Ncokazi K, Chibale K. Reversed chloroquines based on the 3,4-dihydropyrimidin-2(1H)-one scaffold: Synthesis and evaluation for antimalarial, β-haematin inhibition, and cytotoxic activity Chemmedchem. 3: 1649-1653. PMID 18846586 DOI: 10.1002/Cmdc.200800172  0.427
2008 Mahajan A, Kumar V, Mansour NR, Bickle Q, Chibale K. Meclonazepam analogues as potential new antihelmintic agents. Bioorganic & Medicinal Chemistry Letters. 18: 2333-6. PMID 18343662 DOI: 10.1016/J.Bmcl.2008.02.077  0.366
2008 Blackie MA, Saravanamuthu A, Fairlamb AH, Chibale K. Inhibition of trypanothione reductase and glutathione reductase by ferrocenic 4-aminoquinoline ureas Arkivoc. 2008: 52-60. DOI: 10.3998/Ark.5550190.0009.605  0.403
2007 Biot C, Pradines B, Sergeant MH, Gut J, Rosenthal PJ, Chibale K. Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues. Bioorganic & Medicinal Chemistry Letters. 17: 6434-8. PMID 17949976 DOI: 10.1016/J.Bmcl.2007.10.003  0.412
2007 Mahajan A, Yeh S, Nell M, van Rensburg CEJ, Chibale K. Synthesis of new 7-chloroquinolinyl thioureas and their biological investigation as potential antimalarial and anticancer agents Bioorganic and Medicinal Chemistry Letters. 17: 5683-5685. PMID 17768052 DOI: 10.1016/j.bmcl.2007.07.049  0.357
2007 Blackie MAL, Beagley P, Croft SL, Kendrick H, Moss JR, Chibale K. Metallocene-based antimalarials: An exploration into the influence of the ferrocenyl moiety on in vitro antimalarial activity in chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum Bioorganic and Medicinal Chemistry. 15: 6510-6516. PMID 17693090 DOI: 10.1016/J.Bmc.2007.07.012  0.446
2007 Musonda CC, Little S, Yardley V, Chibale K. Application of multicomponent reactions to antimalarial drug discovery. Part 3: discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro. Bioorganic & Medicinal Chemistry Letters. 17: 4733-6. PMID 17644333 DOI: 10.1016/J.Bmcl.2007.06.070  0.465
2007 Pillay P, Vleggaar R, Maharaj VJ, Smith PJ, Lategan CA, Chouteau F, Chibale K. Antiplasmodial hirsutinolides from Vernonia staehelinoides and their utilization towards a simplified pharmacophore. Phytochemistry. 68: 1200-5. PMID 17408709 DOI: 10.1016/J.Phytochem.2007.02.019  0.388
2007 Mbewe B, Chibale K, McIntosh DB. Purification of human malaria parasite hypoxanthine guanine xanthine phosphoribosyltransferase (HGXPRT) using immobilized Reactive Red 120. Protein Expression and Purification. 52: 153-8. PMID 17097304 DOI: 10.1016/J.Pep.2006.09.014  0.31
2007 Chibale K, Stevens A, Bull J. Chemoselectivity and Unusual Internal Acetal Formation in the Synthesis of a Glycosidation Precursor Synlett. 2007: 3175-3179. DOI: 10.1055/S-2007-990910  0.308
2006 Ott R, Chibale K, Anderson S, Chipeleme A, Chaudhuri M, Guerrah A, Colowick N, Hill GC. Novel inhibitors of the trypanosome alternative oxidase inhibit Trypanosoma brucei brucei growth and respiration. Acta Tropica. 100: 172-84. PMID 17126803 DOI: 10.1016/J.Actatropica.2006.10.005  0.412
2006 Chipeleme A, Gut J, Rosenthal PJ, Chibale K. Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum. Bioorganic & Medicinal Chemistry. 15: 273-82. PMID 17052908 DOI: 10.1016/J.Bmc.2006.09.055  0.437
2006 Biot C, Chibale K. Novel approaches to antimalarial drug discovery. Infectious Disorders Drug Targets. 6: 173-204. PMID 16789878 DOI: 10.2174/187152606784112155  0.351
2006 Yeh S, Smith PJ, Chibale K. Dual-acting diamine antiplasmodial and chloroquine resistance modulating agents. Biochemical Pharmacology. 72: 156-65. PMID 16730664 DOI: 10.1016/J.Bcp.2006.04.006  0.412
2006 Musonda CC, Gut J, Rosenthal PJ, Yardley V, Carvalho de Souza RC, Chibale K. Application of multicomponent reactions to antimalarial drug discovery. Part 2: New antiplasmodial and antitrypanosomal 4-aminoquinoline gamma- and delta-lactams via a 'catch and release' protocol. Bioorganic & Medicinal Chemistry. 14: 5605-15. PMID 16690319 DOI: 10.1016/J.Bmc.2006.04.035  0.451
2006 Redelinghuys P, Nchinda AT, Chibale K, Sturrock ED. Novel ketomethylene inhibitors of angiotensin I-converting enzyme (ACE): inhibition and molecular modelling. Biological Chemistry. 387: 461-6. PMID 16606345 DOI: 10.1515/Bc.2006.061  0.315
2005 Chouteau F, Ramanitrahasimbola D, Rasoanaivo P, Chibale K. Exploiting a basic chemosensitizing pharmacophore hypothesis. Part 1: synthesis and biological evaluation of novel arylbromide and bicyclic chemosensitizers against drug-resistant malaria parasites. Bioorganic & Medicinal Chemistry Letters. 15: 3024-8. PMID 15908208 DOI: 10.1016/J.BMCL.2005.04.033  0.339
2005 Chiyanzu I, Clarkson C, Smith PJ, Lehman J, Gut J, Rosenthal PJ, Chibale K. Design, synthesis and anti-plasmodial evaluation in vitro of new 4-aminoquinoline isatin derivatives. Bioorganic & Medicinal Chemistry. 13: 3249-61. PMID 15809160 DOI: 10.1016/J.Bmc.2005.02.037  0.455
2005 Musonda CC, Chibale K. Application of combinatorial and parallel synthesis chemistry methodologies to antiparasitic drug discovery. Current Medicinal Chemistry. 11: 2519-33. PMID 15544460 DOI: 10.2174/0929867043364469  0.352
2005 Musonda CC, Taylor D, Lehman J, Gut J, Rosenthal PJ, Chibale K. Application of multi-component reactions to antimalarial drug discovery. Part 1: Parallel synthesis and antiplasmodial activity of new 4-aminoquinoline Ugi adducts. Bioorganic & Medicinal Chemistry Letters. 14: 3901-5. PMID 15225694 DOI: 10.1016/J.BMCL.2004.05.063  0.35
2004 Greenbaum DC, Mackey Z, Hansell E, Doyle P, Gut J, Caffrey CR, Lehrman J, Rosenthal PJ, McKerrow JH, Chibale K. Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi. Journal of Medicinal Chemistry. 47: 3212-9. PMID 15163200 DOI: 10.1021/Jm030549J  0.43
2004 Chibale K, Musonda CC. The synthesis of parasitic cysteine protease and trypanothione reductase inhibitors. Current Medicinal Chemistry. 10: 1863-89. PMID 12871109 DOI: 10.2174/0929867033456963  0.338
2004 Blackie MA, Beagley P, Chibale K, Clarkson C, Hutton AT, Moss JR, Smith PJ. Corrigendum to “Synthesis and antimalarial activity in vitro of new heterobimetallic complexes: Rh and Au derivatives of chloroquine and a series of ferrocenyl-4-amino-7-chloroquinolines” [Journal of Organometallic Chemistry 688 (2003) 144–152] Journal of Organometallic Chemistry. 689: 1865. DOI: 10.1016/J.Jorganchem.2004.03.004  0.356
2003 Chiyanzu I, Hansell E, Gut J, Rosenthal PJ, McKerrow JH, Chibale K. Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain Bioorganic and Medicinal Chemistry Letters. 13: 3527-3530. PMID 14505663 DOI: 10.1016/S0960-894X(03)00756-X  0.419
2003 Clarkson C, Musonda CC, Chibale K, Campbell WE, Smith P. Synthesis of totarol amino alcohol derivatives and their antiplasmodial activity and cytotoxicity. Bioorganic & Medicinal Chemistry. 11: 4417-22. PMID 13129578 DOI: 10.1016/S0968-0896(03)00491-7  0.457
2003 Chibale K. A chemical approach towards understanding the mechanism and reversal of drug resistance in Plasmodium falciparum: is it viable? Iubmb Life. 53: 249-52. PMID 12121004 DOI: 10.1080/15216540212655  0.321
2003 Chibale K. Towards broadspectrum antiprotozoal agents Arkivoc. 2002: 93-98. DOI: 10.3998/Ark.5550190.0003.910  0.341
2003 Beagley P, Blackie MAL, Chibale K, Clarkson C, Meijboom R, Moss JR, Smith PJ, Su H. Synthesis and antiplasmodial activity in vitro of new ferrocenechloroquine analogues Dalton Transactions. 3046-3051. DOI: 10.1039/B303335J  0.375
2003 Chibale K, Visser M, van Schalkwyk D, Smith PJ, Saravanamuthu A, Fairlamb AH. Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents Tetrahedron. 59: 2289-2296. DOI: 10.1016/S0040-4020(03)00240-0  0.41
2003 Blackie MAL, Beagley P, Chibale K, Clarkson C, Moss JR, Smith PJ. Synthesis and antimalarial activity in vitro of new heterobimetallic complexes: Rh and Au derivatives of chloroquine and a series of ferrocenyl-4-amino-7-chloroquinolines Journal of Organometallic Chemistry. 688: 144-152. DOI: 10.1016/J.Jorganchem.2003.07.026  0.317
2002 Beagley P, Blackie MAL, Chibale K, Clarkson C, Moss JR, Smith PJ. Synthesis and antimalarial activity in vitro of new ruthenocene-chloroquine analogues Journal of the Chemical Society, Dalton Transactions. 4426-4433. DOI: 10.1039/B205432A  0.441
2002 Chibale K, Chipeleme A, Warren S. Convenient synthesis of disulfide substrates for trypanothione reductase using polymer-supported reagents Tetrahedron Letters. 43: 1587-1589. DOI: 10.1016/S0040-4039(02)00064-3  0.582
2001 Chibale K, Haupt H, Kendrick H, Yardley V, Saravanamuthu A, Fairlamb AH, Croft SL. Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine. Bioorganic & Medicinal Chemistry Letters. 11: 2655-7. PMID 11551771 DOI: 10.1016/S0960-894X(01)00528-5  0.442
2001 Chibale K, Ojima I, Haupt H, Geng X, Pera P, Bernacki RJ. Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides. Bioorganic & Medicinal Chemistry Letters. 11: 2457-60. PMID 11549446 DOI: 10.1016/S0960-894X(01)00462-0  0.396
2000 Chibale K, Visser M, Yardley V, Croft SL, Fairlamb AH. Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani. Bioorganic & Medicinal Chemistry Letters. 10: 1147-50. PMID 10866368 DOI: 10.1016/S0960-894X(00)00154-2  0.306
2000 Chibale K, Moss JR, Blackie M, van Schalkwyk D, Smith PJ. New amine and urea analogs of ferrochloroquine: synthesis, antimalarial activity in vitro and electrochemical studies Tetrahedron Letters. 41: 6231-6235. DOI: 10.1016/S0040-4039(00)01036-4  0.366
1998 Nicolaou KC, Trujillo JI, Jandeleit B, Chibale K, Rosenfeld M, Diefenbach B, Cheresh DA, Goodman SL. Design, synthesis and biological evaluation of nonpeptide integrin antagonists Bioorganic and Medicinal Chemistry. 6: 1185-1208. PMID 9784861 DOI: 10.1016/S0968-0896(98)00090-X  0.466
1997 Nicolaou K, Trujillo JI, Chibale K. Design, synthesis and biological evaluation of carbohydrate-based mimetics of cRGDFV Tetrahedron. 53: 8751-8778. DOI: 10.1016/S0040-4020(97)90389-6  0.399
1996 Chibale K, Warren S. Kinetic resolution in asymmetric anti aldol reactions of branched and straight chain racemic 2-phenylsulfanyl aldehydes: asymmetric synthesis of cyclic ethers and lactones by phenylsulfanyl migration Journal of the Chemical Society-Perkin Transactions 1. 1935-1940. DOI: 10.1039/P19960001935  0.595
1995 Chibale K, Warren S. Asymmetric aldol reactions of achiral 2-phenylsulfanyl aldehydes with small- and medium-sized carbocyclic rings: the synthesis of homochiral spirocyclic lactones, pyrrolidines and tetrahydrofurans Journal of the Chemical Society-Perkin Transactions 1. 2411-2418. DOI: 10.1039/P19950002411  0.63
1994 Chibale K, Warren S. The synthesis of optically active 2-phenylthio aldehydes Tetrahedron Letters. 35: 3991-3994. DOI: 10.1016/S0040-4039(00)76722-0  0.588
1993 Chibale K, Warren S. Kinetic Resolutions in Anti Aldol Reactions: Asymmetric Synthesis of Heterocycles with Phenylthio Migration Phosphorus, Sulfur, and Silicon and the Related Elements. 74: 401-402. DOI: 10.1080/10426509308038135  0.607
1993 Chibale K, Greeves N, Lyford L, Pease JE. New homochiral binaphthol-modified organolanthanide reagents for the enantioselective addition to aldehydes Tetrahedron: Asymmetry. 4: 2407-2410. DOI: 10.1016/S0957-4166(00)82211-9  0.752
1993 Chibale K, Hartley RC, Jenkins KP, Simons M, Warren S, Richards IC. The stereochemically controlled synthesis of spirocyclic ethers and lactones with medium-sized (7-, 8-, and 12-membered) carbocyclic rings by phenylthio migration: 1-oxaspiro[4.n]alkanes and alkan-2-ones with n = 6, 7, and 11. Tetrahedron Letters. 34: 6783-6786. DOI: 10.1016/S0040-4039(00)61701-X  0.596
1992 Chibale K, Warren S. Kinetic resolutions in anti aldol reactions with racemic 2-phenylthio aldehydes: asymmetric synthesis of cyclic ethers and lactones with phenylthio migration Tetrahedron Letters. 33: 4369-4372. DOI: 10.1016/S0040-4039(00)74262-6  0.592
1991 Chibale K, Warren S. Asymmetric synthesis of spirocyclic pyrrolidines and tetrahydrofurans by chiral aldol reactions and phenylthio migration Tetrahedron Letters. 32: 6645-6648. DOI: 10.1016/0040-4039(91)80244-Z  0.614
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