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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: thomas s. 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
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. Among authors: thomas s. J Med Chem. 2007 Jun 28;50(13):2990-3003. doi: 10.1021/jm0701019. Epub 2007 May 25. J Med Chem. 2007. PMID: 17523610
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.
Thomas SA, Li T, Woods KW, Song X, Packard G, Fischer JP, Diebold RB, Liu X, Shi Y, Klinghofer V, Johnson EF, Bouska JJ, Olson A, Guan R, Magnone SR, Marsh K, Luo Y, Rosenberg SH, Giranda VL, Li Q. Thomas SA, et al. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3740-4. doi: 10.1016/j.bmcl.2006.04.046. Epub 2006 May 5. Bioorg Med Chem Lett. 2006. PMID: 16678413
Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors.
Woods KW, Fischer JP, Claiborne A, Li T, Thomas SA, Zhu GD, Diebold RB, Liu X, Shi Y, Klinghofer V, Han EK, Guan R, Magnone SR, Johnson EF, Bouska JJ, Olson AM, de Jong R, Oltersdorf T, Luo Y, Rosenberg SH, Giranda VL, Li Q. Woods KW, et al. Bioorg Med Chem. 2006 Oct 15;14(20):6832-46. doi: 10.1016/j.bmc.2006.06.047. Epub 2006 Jul 14. Bioorg Med Chem. 2006. PMID: 16843670
Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.
Zhu GD, Gong J, Claiborne A, Woods KW, Gandhi VB, Thomas S, Luo Y, Liu X, Shi Y, Guan R, Magnone SR, Klinghofer V, Johnson EF, Bouska J, Shoemaker A, Oleksijew A, Stoll VS, De Jong R, Oltersdorf T, Li Q, Rosenberg SH, Giranda VL. Zhu GD, et al. Among authors: thomas s. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3150-5. doi: 10.1016/j.bmcl.2006.03.041. Epub 2006 Apr 5. Bioorg Med Chem Lett. 2006. PMID: 16603355
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: thomas s. 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
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: thomas s. 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
Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.
Tong Y, Stewart KD, Thomas S, Przytulinska M, Johnson EF, Klinghofer V, Leverson J, McCall O, Soni NB, Luo Y, Lin NH, Sowin TJ, Giranda VL, Penning TD. Tong Y, et al. Among authors: thomas s. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5206-8. doi: 10.1016/j.bmcl.2008.08.079. Epub 2008 Aug 28. Bioorg Med Chem Lett. 2008. PMID: 18790640
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