Year |
Citation |
Score |
2022 |
Zhang L, Moccia M, Briggs DC, Bharate JB, Lakkaniga NR, Knowles P, Yan W, Tran P, Kharbanda A, Wang X, Leung YK, Frett B, Santoro M, McDonald NQ, Carlomagno F, et al. Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. Journal of Medicinal Chemistry. 65: 1536-1551. PMID 35081714 DOI: 10.1021/acs.jmedchem.1c01280 |
0.677 |
|
2021 |
Zhang L, Lakkaniga NR, Bharate JB, Mcconnell N, Wang X, Kharbanda A, Leung YK, Frett B, Shah NP, Li HY. Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor. European Journal of Medicinal Chemistry. 225: 113776. PMID 34479037 DOI: 10.1016/j.ejmech.2021.113776 |
0.674 |
|
2021 |
Kharbanda A, Tran P, Zhang L, Leung YK, Li HY, Frett B. Discovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology. European Journal of Medicinal Chemistry. 225: 113763. PMID 34419892 DOI: 10.1016/j.ejmech.2021.113763 |
0.513 |
|
2021 |
Saha D, Ryan KR, Lakkaniga NR, Acharya B, Garcia NG, Smith EL, Frett B. Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. Journal of Medicinal Chemistry. PMID 34402300 DOI: 10.1021/acs.jmedchem.0c02167 |
0.419 |
|
2021 |
Moccia M, Yang D, Lakkaniga NR, Frett B, McConnell N, Zhang L, Brescia A, Federico G, Zhang L, Salerno P, Santoro M, Li HY, Carlomagno F. Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases. Scientific Reports. 11: 16103. PMID 34373541 DOI: 10.1038/s41598-021-95612-4 |
0.531 |
|
2021 |
Kharbanda A, Zhang L, Saha D, Tran P, Xu K, Li MO, Leung YK, Frett B, Li HY. Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors. European Journal of Medicinal Chemistry. 223: 113660. PMID 34246853 DOI: 10.1016/j.ejmech.2021.113660 |
0.541 |
|
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 |
0.501 |
|
2021 |
Frett B, Saha D, Ryan KR, Lakkaniga NR, Smith EL. Pyrazoloadenine Inhibitors of the RET Lung Cancer Oncoprotein Discovered via a Fragment Optimization Approach. Chemmedchem. PMID 33559353 DOI: 10.1002/cmdc.202100013 |
0.318 |
|
2020 |
Wang J, Cheng P, Pavlyukov MS, Yu H, Zhang Z, Kim SH, Minata M, Mohyeldin A, Xie W, Chen D, Goidts V, Frett B, Hu W, Li H, Shin YJ, et al. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2. The Journal of Clinical Investigation. PMID 33044225 DOI: 10.1172/JCI144618 |
0.333 |
|
2020 |
Wang J, Cheng P, Pavlyukov MS, Yu H, Zhang Z, Kim SH, Minata M, Mohyeldin A, Xie W, Chen D, Goidts V, Frett B, Hu W, Li H, Shin YJ, et al. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2. The Journal of Clinical Investigation. 130: 5027. PMID 32870163 DOI: 10.1172/JCI142404 |
0.333 |
|
2020 |
Yan W, Lakkaniga NR, Carlomagno F, Santoro M, McDonald NQ, Lv F, Gunaganti N, Frett B, Li HY. Correction to Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. Journal of Medicinal Chemistry. PMID 32841014 DOI: 10.1021/Acs.Jmedchem.0C01351 |
0.459 |
|
2020 |
Lakkaniga NR, Gunaganti N, Zhang L, Belachew B, Frett B, Leung YK, Li HY. Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of RET: Design, synthesis and biological evaluation. European Journal of Medicinal Chemistry. 206: 112691. PMID 32823007 DOI: 10.1016/J.Ejmech.2020.112691 |
0.517 |
|
2020 |
Lakkaniga NR, Zhang L, Belachew B, Gunaganti N, Frett B, Li HY. Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression. European Journal of Medicinal Chemistry. 203: 112589. PMID 32717530 DOI: 10.1016/j.ejmech.2020.112589 |
0.515 |
|
2020 |
Storey AJ, Naceanceno KS, Lan RS, Washam CL, Orr LM, Mackintosh SG, Tackett AJ, Edmondson RD, Wang Z, Li HY, Frett B, Kendrick S, Byrum SD. ProteoViz: a tool for the analysis and interactive visualization of phosphoproteomics data. Molecular Omics. PMID 32347222 DOI: 10.1039/c9mo00149b |
0.364 |
|
2020 |
Moccia M, Frett B, Zhang L, Lakkaniga NR, Briggs DC, Chauhan R, Brescia A, Federico G, Yan W, Santoro M, McDonald NQ, Li HY, Carlomagno F. Bioisosteric discovery of NPA101.3, a second generation RET/VEGFR2 inhibitor optimized for single-agent polypharmacology. Journal of Medicinal Chemistry. PMID 32298114 DOI: 10.1021/Acs.Jmedchem.9B01336 |
0.526 |
|
2020 |
Lei J, Song GT, He LJ, Luo YF, Tang DY, Lin HK, Frett B, Li HY, Chen ZZ, Xu ZG. One-pot construction of functionalized aziridines and maleimides via a novel pseudo-Knoevenagel cascade reaction. Chemical Communications (Cambridge, England). PMID 31971170 DOI: 10.1039/C9Cc08220D |
0.406 |
|
2019 |
Lakkaniga NR, Balasubramaniam M, Zhang S, Frett B, Li HY. Structural Characterization of the Aurora Kinase B "DFG-flip" Using Metadynamics. The Aaps Journal. 22: 14. PMID 31853739 DOI: 10.1208/s12248-019-0399-6 |
0.409 |
|
2019 |
Saha D, Kharbanda A, Yan W, Lakkaniga NR, Frett B, Li HY. The Exploration of Chirality for Improved Druggability within the Human Kinome. Journal of Medicinal Chemistry. PMID 31550151 DOI: 10.1021/acs.jmedchem.9b00640 |
0.489 |
|
2018 |
Gunaganti N, Kharbanda A, Lakkaniga NR, Zhang L, Cooper R, Li HY, Frett B. Catalyst free, C-3 functionalization of imidazo[1,2-a]pyridines to rapidly access new chemical space for drug discovery efforts. Chemical Communications (Cambridge, England). PMID 30375586 DOI: 10.1039/c8cc07063f |
0.359 |
|
2018 |
Frett B, McConnell N, Kharbanda A, Naresh G, Rounseville B, Warner C, Chang J, Debolske N, Li HY. Selective, C-3 Friedel-Crafts acylation to generate functionally diverse, acetylated Imidazo[1,2-]pyridine derivatives. Tetrahedron. 74: 4592-4600. PMID 30344351 DOI: 10.1016/J.Tet.2018.07.027 |
0.358 |
|
2018 |
Yan W, Lakkaniga NR, Carlomangno F, Santoro M, McDonald N, Lv F, Gunaganti N, Frett B, Li HY. Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. Journal of Medicinal Chemistry. PMID 30188734 DOI: 10.1021/Acs.Jmedchem.8B01092 |
0.5 |
|
2018 |
He LJ, Yang DL, Li SQ, Zhang YJ, Tang Y, Lei J, Frett B, Lin HK, Li HY, Chen ZZ, Xu ZG. Facile construction of fused benzimidazole-isoquinolinones that induce cell-cycle arrest and apoptosis in colorectal cancer cells. Bioorganic & Medicinal Chemistry. PMID 29921474 DOI: 10.1016/j.bmc.2018.06.010 |
0.452 |
|
2018 |
Bharate JB, McConnell N, Naresh G, Zhang L, Lakkaniga NR, Ding L, Shah NP, Frett B, Li HY. Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. Scientific Reports. 8: 3722. PMID 29487300 DOI: 10.1038/S41598-018-21839-3 |
0.537 |
|
2017 |
McConnell N, Xu Z, Kumarasamy V, Sun D, Frett B, Li HY. Synthesis of Constrained Heterocycles Employing Two Post-Ugi Cyclization Methods for Rapid Library Generation with In Cellulo Activity. Chemistryselect. 2: 11821-11825. PMID 30140731 DOI: 10.1002/slct.201702179 |
0.414 |
|
2017 |
Wang J, Cheng P, Pavlyukov MS, Yu H, Zhang Z, Kim SH, Minata M, Mohyeldin A, Xie W, Chen D, Goidts V, Frett B, Hu W, Li H, Shin YJ, et al. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2. The Journal of Clinical Investigation. PMID 28737508 DOI: 10.1172/Jci89092 |
0.477 |
|
2016 |
Xi JB, Fang YF, Frett B, Zhu ML, Zhu T, Kong YN, Guan FJ, Zhao Y, Zhang XW, Li HY, Ma ML, Hu W. Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities. European Journal of Medicinal Chemistry. 126: 1083-1106. PMID 28039836 DOI: 10.1016/J.Ejmech.2016.12.026 |
0.494 |
|
2015 |
Frett B, Carlomagno F, Moccia ML, Brescia A, Federico G, De Falco V, Admire B, Chen Z, Qi W, Santoro M, Li HY. Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology. Angewandte Chemie (International Ed. in English). 54: 8717-21. PMID 26126987 DOI: 10.1002/anie.201501104 |
0.545 |
|
2015 |
Frett B, McConnell N, Smith CC, Wang Y, Shah NP, Li HY. Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors. European Journal of Medicinal Chemistry. 94: 123-31. PMID 25765758 DOI: 10.1016/J.Ejmech.2015.02.052 |
0.552 |
|
2014 |
Frett B, McConnell N, Wang Y, Xu Z, Ambrose A, Li HY. Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies. Medchemcomm. 5: 1507-1514. PMID 26843921 DOI: 10.1039/C4MD00251B |
0.496 |
|
2014 |
Frett B, Moccia M, Carlomagno F, Santoro M, Li HY. Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation. European Journal of Medicinal Chemistry. 86: 714-23. PMID 25232968 DOI: 10.1016/j.ejmech.2014.09.023 |
0.493 |
|
2014 |
Frett B, Brown RV, Ma M, Hu W, Han H, Li HY. Therapeutic melting pot of never in mitosis gene a related kinase 2 (Nek2): a perspective on Nek2 as an oncology target and recent advancements in Nek2 small molecule inhibition. Journal of Medicinal Chemistry. 57: 5835-44. PMID 24517277 DOI: 10.1021/jm401719n |
0.47 |
|
2013 |
Wang Y, Kaiser CE, Frett B, Li HY. Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators. Journal of Medicinal Chemistry. 56: 5219-30. PMID 23566315 DOI: 10.1021/jm3017706 |
0.38 |
|
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