Ernst ter Haar, Ph.D. - Related publications

Vertex Pharmaceuticals, Boston, MA, United States 
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50 most relevant papers in past 60 days:
Year Citation  Score
2021 Singh A, Chang TY, Kaur N, Hsu KC, Yen Y, Lin TE, Lai MJ, Lee SB, Liou JP. CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition. European Journal of Medicinal Chemistry. 215: 113169. PMID 33588178 DOI: 10.1016/j.ejmech.2021.113169   
2021 El-Sattar NEAA, Badawy EHK, AbdEl-Hady WH, Abo-Alkasem MI, Mandour AA, Ismail NSM. Design and Synthesis of New CDK2 Inhibitors Containing Thiazolone and Thiazolthione Scafold with Apoptotic Activity. Chemical & Pharmaceutical Bulletin. 69: 106-117. PMID 33390512 DOI: 10.1248/cpb.c20-00714   
2021 Hu J, Zhang Y, Tang N, Lu Y, Guo P, Huang Z. Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR. Bioorganic & Medicinal Chemistry. 32: 115997. PMID 33440319 DOI: 10.1016/j.bmc.2021.115997   
2021 Hu J, Zhang Y, Tang N, Lu Y, Guo P, Huang Z. Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR. Bioorganic & Medicinal Chemistry. 32: 115997. PMID 33440319 DOI: 10.1016/j.bmc.2021.115997   
2021 Ghorab MM, Abdel-Kader MS, Alqahtani AS, Soliman AM. Synthesis of some quinazolinones inspired from the natural alkaloid Lnorephedrine as EGFR inhibitors and radiosensitizers. Journal of Enzyme Inhibition and Medicinal Chemistry. 36: 218-237. PMID 33357002 DOI: 10.1080/14756366.2020.1854243   
2021 Lawal B, Liu YL, Mokgautsi N, Khedkar H, Sumitra MR, Wu ATH, Huang HS. Pharmacoinformatics and Preclinical Studies of NSC765690 and NSC765599, Potential STAT3/CDK2/4/6 Inhibitors with Antitumor Activities against NCI60 Human Tumor Cell Lines. Biomedicines. 9. PMID 33477856 DOI: 10.3390/biomedicines9010092   
2021 Lenis-Rojas OA, Robalo MP, Tomaz AI, Fernandes AR, Roma-Rodrigues C, Teixeira RG, Marques F, Folgueira M, Yáñez J, Gonzalez AA, Salamini-Montemurri M, Pech-Puch D, Vázquez-García D, Torres ML, Fernández A, et al. Half-Sandwich Ru(-cymene) Compounds with Diphosphanes: and Evaluation As Potential Anticancer Metallodrugs. Inorganic Chemistry. PMID 33570919 DOI: 10.1021/acs.inorgchem.0c02768   
2021 Chan PF, Ang KP, Hamid RA. A bismuth diethyldithiocarbamate compound induced apoptosis via mitochondria-dependent pathway and suppressed invasion in MCF-7 breast cancer cells. Biometals : An International Journal On the Role of Metal Ions in Biology, Biochemistry, and Medicine. PMID 33555494 DOI: 10.1007/s10534-021-00286-0   
2021 Qin J, Qu S, Zhu K, Cheng Y, Pan G, Jing W, Liu X, Sun X, Liu L. Rational design and synthesis of 6-aryl-6H-benzo[c]chromenes as non-steroidal progesterone receptor antagonists for use against cancers. Bioorganic & Medicinal Chemistry. 32: 116003. PMID 33461148 DOI: 10.1016/j.bmc.2021.116003   
2021 Elhady SS, Abdelhameed RFA, El-Ayouty MM, Ibrahim AK, Habib ES, Elgawish MS, Hassanean HA, Safo MK, Nafie MS, Ahmed SA. New Antiproliferative Triflavanone from -Isolation, Structure Elucidation and Molecular Docking Studies. Molecules (Basel, Switzerland). 26. PMID 33572651 DOI: 10.3390/molecules26030739   
2021 Nagy MI, Darwish KM, Kishk SM, Tantawy MA, Nasr AM, Qushawy M, Swidan SA, Mostafa SM, Salama I. Design, Synthesis, Anticancer Activity, and Solid Lipid Nanoparticle Formulation of Indole- and Benzimidazole-Based Compounds as Pro-Apoptotic Agents Targeting Bcl-2 Protein. Pharmaceuticals (Basel, Switzerland). 14. PMID 33535550 DOI: 10.3390/ph14020113   
2021 Komuraiah B, Ren Y, Xue M, Cheng B, Liu J, Liu Y, Chen J. Design, Synthesis and Biological Evaluation of Benz-Fused Five-Membered Heterocyclic Compounds as Tubulin Polymerization Inhibitors with Anticancer Activities. Chemical Biology & Drug Design. PMID 33638903 DOI: 10.1111/cbdd.13832   
2021 Ayoub NM, Alkhalifa AE, Ibrahim DR, Alhusban A. Combined crizotinib and endocrine drugs inhibit proliferation, migration, and colony formation of breast cancer cells via downregulation of MET and estrogen receptor. Medical Oncology (Northwood, London, England). 38: 8. PMID 33449292 DOI: 10.1007/s12032-021-01458-1   
2021 Tucker SJ, Zorn AJ. The Role of POPDC1 in the Progression of the Malignant Phenotype. British Journal of Pharmacology. PMID 33533478 DOI: 10.1111/bph.15403   
2021 Zhou WX, Chen C, Liu XQ, Li Y, Kong LY, Luo JG. Synthesis and biological evaluation of novel withangulatin A derivatives as potential anticancer agents. Bioorganic Chemistry. 108: 104690. PMID 33592485 DOI: 10.1016/j.bioorg.2021.104690   
2021 Liu HP, Liao Y, Ren MZ, Quan ZJ, Wang XC. Synthesis, structural characterization, molecular docking study, biological activity of carbon monoxide release molecules as potent antitumor agents. Bioorganic Chemistry. 107: 104621. PMID 33465671 DOI: 10.1016/j.bioorg.2020.104621   
2021 Joshi A, Gupta R, Sharma D, Singh M. A Mo(VI) based coordination polymer as an antiproliferative agent against cancer cells. Dalton Transactions (Cambridge, England : 2003). PMID 33410831 DOI: 10.1039/d0dt03865b   
2021 Hagras M, El Deeb MA, Elzahabi HSA, Elkaeed EB, Mehany ABM, Eissa IH. Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation. Journal of Enzyme Inhibition and Medicinal Chemistry. 36: 640-658. PMID 33588683 DOI: 10.1080/14756366.2021.1883598   
2021 Wang B, Wang LR, Liu LL, Wang W, Man RJ, Zheng DJ, Deng YS, Yang YS, Xu C, Zhu HL. A novel series of benzothiazepine derivatives as tubulin polymerization inhibitors with anti-tumor potency. Bioorganic Chemistry. 108: 104585. PMID 33508676 DOI: 10.1016/j.bioorg.2020.104585   
2021 Zhang J, Chen P, Duan Y, Xiong H, Li H, Zeng Y, Liang G, Tang Q, Wu D. Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidine derivatives containing 1,8-naphthyridine-4-one fragment. European Journal of Medicinal Chemistry. 215: 113273. PMID 33601310 DOI: 10.1016/j.ejmech.2021.113273   
2021 Damghani T, Moosavi F, Khoshneviszadeh M, Mortazavi M, Pirhadi S, Kayani Z, Saso L, Edraki N, Firuzi O. Imidazopyridine hydrazone derivatives exert antiproliferative effect on lung and pancreatic cancer cells and potentially inhibit receptor tyrosine kinases including c-Met. Scientific Reports. 11: 3644. PMID 33574356 DOI: 10.1038/s41598-021-83069-4   
2021 Yan W, Zhang L, Lv F, Moccia M, Carlomagno F, Landry C, Santoro M, Gosselet F, Frett B, Li HY. Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation. European Journal of Medicinal Chemistry. 216: 113265. PMID 33652352 DOI: 10.1016/j.ejmech.2021.113265   
2021 Pradubyat N, Giannoudis A, Elmetwali T, Mahalapbutr P, Palmieri C, Mitrpant C, Ketchart W. 1'-Acetoxychavicol Acetate from Alpinia galanga Represses Proliferation and Invasion, and Induces Apoptosis via HER2-signaling in Endocrine-Resistant Breast Cancer Cells. Planta Medica. PMID 33445186 DOI: 10.1055/a-1307-3997   
2021 Gui C, Zhang C, Xiong X, Huang J, Xi J, Gong L, Huang B, Zhang X. Total flavone extract from Ampelopsis megalophylla induces apoptosis in the MCF‑7 cell line. International Journal of Oncology. PMID 33469684 DOI: 10.3892/ijo.2021.5172   
2021 Das A, Kumar S, Persoons L, Daelemans D, Schols D, Alici H, Tahtaci H, Karki SS. Synthesis, in silico ADME, molecular docking and in vitro cytotoxicity evaluation of stilbene linked 1,2,3-triazoles. Heliyon. 7: e05893. PMID 33553718 DOI: 10.1016/j.heliyon.2020.e05893   
2021 Zhang Y, Li M, Zhang Q, Wang Z, Li X, Bao J, Zhang H. Arthpyrone L, a New Pyridone Alkaloid from a Deep-sea Arthrinium sp., Inhibits Proliferation of MG63 Osteosarcoma Cells by Inducing G0/G1 Arrest and Apoptosis. Chemistry & Biodiversity. PMID 33427403 DOI: 10.1002/cbdv.202000639   
2021 Abdelaal MR, Soror SH, Elnagar MR, Haffez H. Revealing the Potential Application of EC-Synthetic Retinoid Analogues in Anticancer Therapy. Molecules (Basel, Switzerland). 26. PMID 33477997 DOI: 10.3390/molecules26020506   
2021 Yan J, Zhuang Q, Li Z, Xiong Y, He M, Kang C, Zhang Q, Han L, Liang E, Liu H, Ke P, Huang X. MIL-1, a novel antitumor agent derived from natural product millepachine, acts as tubulin polymerization inhibitor for the treatment of hepatocellular carcinoma. European Journal of Pharmacology. 173975. PMID 33647258 DOI: 10.1016/j.ejphar.2021.173975   
2021 Voloshina AD, Sapunova AS, Kulik NV, Belenok MG, Strobykina IY, Lyubina AP, Gumerova SK, Kataev VE. Antimicrobial and cytotoxic effects of ammonium derivatives of diterpenoids steviol and isosteviol. Bioorganic & Medicinal Chemistry. 32: 115974. PMID 33461146 DOI: 10.1016/j.bmc.2020.115974   
2021 Sun Y, Yin E, Tan Y, Yang T, Song D, Jin S, Guo Z, Wang X. Immunogenicity and cytotoxicity of a platinum(IV) complex derived from capsaicin. Dalton Transactions (Cambridge, England : 2003). PMID 33433537 DOI: 10.1039/d0dt03470c   
2021 Liu Q, Liu Z, Hua W, Gou S. Discovery of 6-(7-Nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol Derivatives as Glutathione Transferase Inhibitors with Favorable Selectivity and Tolerated Toxicity. Journal of Medicinal Chemistry. PMID 33529017 DOI: 10.1021/acs.jmedchem.0c02048   
2021 Chrobak E, Jastrzębska M, Bębenek E, Kadela-Tomanek M, Marciniec K, Latocha M, Wrzalik R, Kusz J, Boryczka S. Molecular Structure, In Vitro Anticancer Study and Molecular Docking of New Phosphate Derivatives of Betulin. Molecules (Basel, Switzerland). 26. PMID 33572631 DOI: 10.3390/molecules26030737   
2021 El Azab IH, El-Sheshtawy HS, Bakr RB, Elkanzi NAA. New 1,2,3-Triazole-Containing Hybrids as Antitumor Candidates: Design, Click Reaction Synthesis, DFT Calculations, and Molecular Docking Study. Molecules (Basel, Switzerland). 26. PMID 33573040 DOI: 10.3390/molecules26030708   
2021 Chen T, Yang P, Chen HJ, Huang B. A new biflavonoids from induced non-apoptotic cell death in A549 cells. Natural Product Research. 1-7. PMID 33615932 DOI: 10.1080/14786419.2021.1882456   
2021 Go RE, Kim CW, Lee SM, Lee HK, Choi KC. Fenhexamid induces cancer growth and survival via estrogen receptor-dependent and PI3K-dependent pathways in breast cancer models. Food and Chemical Toxicology : An International Journal Published For the British Industrial Biological Research Association. 112000. PMID 33484789 DOI: 10.1016/j.fct.2021.112000   
2021 Andima M, Ndakala A, Derese S, Biswajyoti S, Hussain A, Yang LJ, Akoth OE, Coghi P, Pal C, Heydenreich M, Wong VK, Yenesew A. Antileishmanial and cytotoxic activity of secondary metabolites from and two species. Natural Product Research. 1-5. PMID 33459049 DOI: 10.1080/14786419.2021.1871906   
2021 Shakil MS, Parveen S, Rana Z, Walsh F, Movassaghi S, Söhnel T, Azam M, Shaheen MA, Jamieson SMF, Hanif M, Rosengren RJ, Hartinger CG. High Antiproliferative Activity of Hydroxythiopyridones over Hydroxypyridones and Their Organoruthenium Complexes. Biomedicines. 9. PMID 33513800 DOI: 10.3390/biomedicines9020123   
2021 Sequeira D, Baptista PV, Valente R, Piedade MFM, Garcia MH, Morais TS, Fernandes AR. Cu(I) complexes as new antiproliferative agents against sensitive and doxorubicin resistant colorectal cancer cells: synthesis, characterization, and mechanisms of action. Dalton Transactions (Cambridge, England : 2003). PMID 33470993 DOI: 10.1039/d0dt03566a   
2021 Lee SE, Sivtseva S, Lim C, Okhlopkova Z, Cho S. Artemisia kruhsiana leaf extract induces autophagic cell death in human prostate cancer cells. Chinese Journal of Natural Medicines. 19: 134-142. PMID 33641784 DOI: 10.1016/S1875-5364(21)60014-6   
2021 Zheng L, Gao T, Ge Z, Ma Z, Xu J, Ding W, Shen L. Design, Synthesis and Structure-Activity Relationship Studies of Glycosylated Derivatives of Marine Natural Product Lamellarin D. European Journal of Medicinal Chemistry. 214: 113226. PMID 33582387 DOI: 10.1016/j.ejmech.2021.113226   
2021 Marquez J, Dong J, Dong C, Tian C, Serrero G. Identification of Prostaglandin F2 Receptor Negative Regulator (PTGFRN) as an internalizable target in cancer cells for antibody-drug conjugate development. Plos One. 16: e0246197. PMID 33503070 DOI: 10.1371/journal.pone.0246197   
2021 Terasaki M, Takahashi S, Nishimura R, Kubota A, Kojima H, Ohta T, Hamada J, Kuramitsu Y, Maeda H, Miyashita K, Takahashi M, Mutoh M. A Marine Carotenoid of Fucoxanthinol Accelerates the Growth of Human Pancreatic Cancer PANC-1 Cells. Nutrition and Cancer. 1-16. PMID 33590779 DOI: 10.1080/01635581.2020.1863994   
2021 Mokhir A, Xu H, Schikora M, Sisa M, Daum S, Janko C, Alexiou C, Bilyy R, Klemt I, Sellner L, Gong W, Schmitt M, Bila G. An endoplasmic reticulum - specific pro-amplifier of reactive oxygen species in cancer cells. Angewandte Chemie (International Ed. in English). PMID 33656236 DOI: 10.1002/anie.202100054   
2021 Yang G, Xing J, Aikemu B, Sun J, Zheng M. Kaempferol exhibits a synergistic effect with doxorubicin to inhibit proliferation, migration, and invasion of liver cancer. Oncology Reports. 45. PMID 33649865 DOI: 10.3892/or.2021.7983   
2021 Cohen-Sharir Y, McFarland JM, Abdusamad M, Marquis C, Bernhard SV, Kazachkova M, Tang H, Ippolito MR, Laue K, Zerbib J, Malaby HLH, Jones A, Stautmeister LM, Bockaj I, Wardenaar R, et al. Aneuploidy renders cancer cells vulnerable to mitotic checkpoint inhibition. Nature. PMID 33505028 DOI: 10.1038/s41586-020-03114-6   
2021 Kang SU, Kim DH, Lee YS, Huang M, Byeon HK, Lee SH, Baek SJ, Kim CH. DIM-C-pPhtBu induces lysosomal dysfunction and unfolded protein response -mediated cell death via excessive mitophagy. Cancer Letters. PMID 33556544 DOI: 10.1016/j.canlet.2021.01.005   
2021 Machalz D, Li H, Du W, Sharma S, Liu S, Bureik M, Wolber G. Discovery of a novel potent cytochrome P450 CYP4Z1 inhibitor. European Journal of Medicinal Chemistry. 215: 113255. PMID 33611185 DOI: 10.1016/j.ejmech.2021.113255   
2021 Gao XZ, Lv XT, Zhang RR, Luo Y, Wang MX, Chen JS, Zhang YK, Sun B, Sun JY, Liu YF, Liu C. Design, synthesis and in vitro anticancer research of novel tetrandrine and fangchinoline derivatives. Bioorganic Chemistry. 109: 104694. PMID 33601141 DOI: 10.1016/j.bioorg.2021.104694   
2021 Wang WY, Wu WY, Li AL, Liu QS, Sun Y, Gu W. Synthesis, anticancer evaluation and mechanism studies of novel indolequinone derivatives of ursolic acid. Bioorganic Chemistry. 109: 104705. PMID 33618252 DOI: 10.1016/j.bioorg.2021.104705   
2021 Tantak MP, Malik M, Klingler L, Olson Z, Kumar A, Sadana R, Kumar D. Indolyl-α-keto-1,3,4-oxadiazoles: synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerization. Bioorganic & Medicinal Chemistry Letters. 127842. PMID 33556575 DOI: 10.1016/j.bmcl.2021.127842