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Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).
Wehn PM, Rizzi JP, Dixon DD, Grina JA, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Cao Z, Cheng T, Czerwinski RM, Goggin BS, Huang H, Halfmann MM, Maddie MA, Morton EL, Olive SR, Tan H, Xie S, Wong T, Josey JA, Wallace EM. Wehn PM, et al. Among authors: wang k, wang b. J Med Chem. 2018 Nov 8;61(21):9691-9721. doi: 10.1021/acs.jmedchem.8b01196. Epub 2018 Oct 18. J Med Chem. 2018. PMID: 30289716
3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.
Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD, Czerwinski RM, Du X, Ged EL, Han G, Tan H, Wong T, Xie S, Josey JA, Wallace EM. Xu R, et al. Among authors: wang k, wang b. J Med Chem. 2019 Aug 8;62(15):6876-6893. doi: 10.1021/acs.jmedchem.9b00719. Epub 2019 Jul 8. J Med Chem. 2019. PMID: 31282155 Clinical Trial.
A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma.
Wallace EM, Rizzi JP, Han G, Wehn PM, Cao Z, Du X, Cheng T, Czerwinski RM, Dixon DD, Goggin BS, Grina JA, Halfmann MM, Maddie MA, Olive SR, Schlachter ST, Tan H, Wang B, Wang K, Xie S, Xu R, Yang H, Josey JA. Wallace EM, et al. Among authors: wang k, wang b. Cancer Res. 2016 Sep 15;76(18):5491-500. doi: 10.1158/0008-5472.CAN-16-0473. Epub 2016 Sep 6. Cancer Res. 2016. PMID: 27635045
Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.
Jiang Y, Andrews SW, Condroski KR, Buckman B, Serebryany V, Wenglowsky S, Kennedy AL, Madduru MR, Wang B, Lyon M, Doherty GA, Woodard BT, Lemieux C, Geck Do M, Zhang H, Ballard J, Vigers G, Brandhuber BJ, Stengel P, Josey JA, Beigelman L, Blatt L, Seiwert SD. Jiang Y, et al. Among authors: wang b. J Med Chem. 2014 Mar 13;57(5):1753-69. doi: 10.1021/jm400164c. Epub 2013 May 28. J Med Chem. 2014. PMID: 23672640
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.
Wang T, Lamb ML, Scott DA, Wang H, Block MH, Lyne PD, Lee JW, Davies AM, Zhang HJ, Zhu Y, Gu F, Han Y, Wang B, Mohr PJ, Kaus RJ, Josey JA, Hoffmann E, Thress K, Macintyre T, Wang H, Omer CA, Yu D. Wang T, et al. Among authors: wang h, wang b. J Med Chem. 2008 Aug 14;51(15):4672-84. doi: 10.1021/jm800343j. Epub 2008 Jul 23. J Med Chem. 2008. PMID: 18646745
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD, MacIntyre T, Mohr PJ, Omer CA, Sjögren T, Thress K, Wang B, Wang H, Yu D, Zhang HJ. Wang T, et al. Among authors: wang h, wang b. ACS Med Chem Lett. 2012 Jul 26;3(9):705-9. doi: 10.1021/ml300074j. eCollection 2012 Sep 13. ACS Med Chem Lett. 2012. PMID: 24900538 Free PMC article.
C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.
Du X, Hinklin RJ, Xiong Y, Dransfield P, Park J, Kohn TJ, Pattaropong V, Lai S, Fu Z, Jiao X, Chow D, Jin L, Davda J, Veniant MM, Anderson DA, Baer BR, Bencsik JR, Boyd SA, Chicarelli MJ, Mohr PJ, Wang B, Condroski KR, DeWolf WE, Conn M, Tran T, Yang J, Aicher TD, Medina JC, Coward P, Houze JB. Du X, et al. Among authors: wang b. ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25516785 Free PMC article.
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