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144 results

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Page 1
Discovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor.
Yu Y, Jang M, Miyashiro J, Clark RF, Zhu GD, Gong J, Dai Y, Frey RR, Penning TD, Kim H, Lee HK, Kim JK, Ryu KM, Park SJ, Yoon T, Li T, Kurnick MD, Kapecki NJ, Li L, Gorman JV, Montgomery DA, Manaves V, Bromberg KD, Doktor SZ, Thakur A, Wang J, Smith HA, Buchanan FG, Ferguson DC, Torrent M, Jakob CG, Qiu W, Upadhyay AK, Martin RL, Lai A, Michaelides MR. Yu Y, et al. Among authors: zhu gd. J Med Chem. 2024 Oct 10;67(19):17000-17032. doi: 10.1021/acs.jmedchem.4c01450. Epub 2024 Sep 16. J Med Chem. 2024. PMID: 39283694
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension.
Zhu GD, Gandhi VB, Gong J, Thomas S, Woods KW, Song X, Li T, Diebold RB, Luo Y, Liu X, Guan R, Klinghofer V, Johnson EF, Bouska J, Olson A, Marsh KC, Stoll VS, Mamo M, Polakowski J, Campbell TJ, Martin RL, Gintant GA, Penning TD, Li Q, Rosenberg SH, Giranda VL. Zhu GD, et al. J Med Chem. 2007 Jun 28;50(13):2990-3003. doi: 10.1021/jm0701019. Epub 2007 May 25. J Med Chem. 2007. PMID: 17523610
Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors.
Tong Y, Florjancic AS, Clark RF, Lai C, Mastracchio A, Zhu GD, Smith ML, Kovar PJ, Shaw B, Albert DH, Qiu W, Longenecker KL, Liu X, Olson AM, Osterling DJ, Tahir SK, Phillips DC, Leverson JD, Souers AJ, Penning TD. Tong Y, et al. Among authors: zhu gd. ACS Med Chem Lett. 2021 Jun 22;12(7):1108-1115. doi: 10.1021/acsmedchemlett.1c00161. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267880 Free PMC article.
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: zhu gd. 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: zhu gd. J Med Chem. 2009 Jan 22;52(2):514-23. doi: 10.1021/jm801171j. J Med Chem. 2009. PMID: 19143569
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.
Li Q, Woods KW, Thomas S, Zhu GD, Packard G, Fisher J, Li T, Gong J, Dinges J, Song X, Abrams J, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Des Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL. Li Q, et al. Among authors: zhu gd. Bioorg Med Chem Lett. 2006 Apr 1;16(7):2000-7. doi: 10.1016/j.bmcl.2005.12.065. Epub 2006 Jan 18. Bioorg Med Chem Lett. 2006. PMID: 16413780
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. 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
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.
Li Q, Li T, Zhu GD, Gong J, Claibone A, Dalton C, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Bauch JL, Marsh KC, Bouska JJ, Arries S, De Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL. Li Q, et al. Among authors: zhu gd. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1679-85. doi: 10.1016/j.bmcl.2005.12.017. Epub 2006 Jan 5. Bioorg Med Chem Lett. 2006. PMID: 16403626
144 results