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Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.
Wang H, Ren B, Liu Y, Jiang B, Guo Y, Wei M, Luo L, Kuang X, Qiu M, Lv L, Xu H, Qi R, Yan H, Xu D, Wang Z, Huo CX, Zhu Y, Zhao Y, Wu Y, Qin Z, Su D, Tang T, Wang F, Sun X, Feng Y, Peng H, Wang X, Gao Y, Liu Y, Gong W, Yu F, Liu X, Wang L, Zhou C. Wang H, et al. Among authors: liu y, liu x. J Med Chem. 2020 Dec 24;63(24):15541-15563. doi: 10.1021/acs.jmedchem.0c01346. Epub 2020 Dec 2. J Med Chem. 2020. PMID: 33264017
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Guo Y, Liu Y, Hu N, Yu D, Zhou C, Shi G, Zhang B, Wei M, Liu J, Luo L, Tang Z, Song H, Guo Y, Liu X, Su D, Zhang S, Song X, Zhou X, Hong Y, Chen S, Cheng Z, Young S, Wei Q, Wang H, Wang Q, Lv L, Wang F, Xu H, Sun H, Xing H, Li N, Zhang W, Wang Z, Liu G, Sun Z, Zhou D, Li W, Liu L, Wang L, Wang Z. Guo Y, et al. Among authors: liu j, liu y, liu x, liu l, liu g. J Med Chem. 2019 Sep 12;62(17):7923-7940. doi: 10.1021/acs.jmedchem.9b00687. Epub 2019 Aug 19. J Med Chem. 2019. PMID: 31381333
Pamiparib is a potent and selective PARP inhibitor with unique potential for the treatment of brain tumor.
Xiong Y, Guo Y, Liu Y, Wang H, Gong W, Liu Y, Wang X, Gao Y, Yu F, Su D, Wang F, Zhu Y, Zhao Y, Wu Y, Qin Z, Sun X, Ren B, Jiang B, Jin W, Shen Z, Tang Z, Song X, Wang L, Liu X, Zhou C, Jiang B. Xiong Y, et al. Among authors: liu y, liu x. Neoplasia. 2020 Sep;22(9):431-440. doi: 10.1016/j.neo.2020.06.009. Epub 2020 Jul 8. Neoplasia. 2020. PMID: 32652442 Free PMC article.
Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Penning TD, Zhu GD, Gandhi VB, Gong J, Thomas S, Lubisch W, Grandel R, Wernet W, Park CH, Fry EH, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Olson AM, Marsh KC, Luo Y, Rosenberg SH, Giranda VL. Penning TD, et al. Among authors: liu x. Bioorg Med Chem. 2008 Jul 15;16(14):6965-75. doi: 10.1016/j.bmc.2008.05.044. Epub 2008 May 27. Bioorg Med Chem. 2008. PMID: 18541433
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
Penning TD, Zhu GD, Gong J, Thomas S, Gandhi VB, Liu X, Shi Y, Klinghofer V, Johnson EF, Park CH, Fry EH, Donawho CK, Frost DJ, Buchanan FG, Bukofzer GT, Rodriguez LE, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL. Penning TD, et al. Among authors: liu x. J Med Chem. 2010 Apr 22;53(8):3142-53. doi: 10.1021/jm901775y. J Med Chem. 2010. PMID: 20337371
Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.
Penning TD, Zhu GD, Gandhi VB, Gong J, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL. Penning TD, et al. Among authors: liu x. J Med Chem. 2009 Jan 22;52(2):514-23. doi: 10.1021/jm801171j. J Med Chem. 2009. PMID: 19143569
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.
Zhu GD, Gandhi VB, Gong J, Thomas S, Luo Y, Liu X, Shi Y, Klinghofer V, Johnson EF, Frost D, Donawho C, Jarvis K, Bouska J, Marsh KC, Rosenberg SH, Giranda VL, Penning TD. Zhu GD, et al. Among authors: liu x. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3955-8. doi: 10.1016/j.bmcl.2008.06.023. Epub 2008 Jun 12. Bioorg Med Chem Lett. 2008. PMID: 18586490
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.
Tong Y, Bouska JJ, Ellis PA, Johnson EF, Leverson J, Liu X, Marcotte PA, Olson AM, Osterling DJ, Przytulinska M, Rodriguez LE, Shi Y, Soni N, Stavropoulos J, Thomas S, Donawho CK, Frost DJ, Luo Y, Giranda VL, Penning TD. Tong Y, et al. Among authors: liu x. J Med Chem. 2009 Nov 12;52(21):6803-13. doi: 10.1021/jm900697r. J Med Chem. 2009. PMID: 19888760
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