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2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Harris CM, Ericsson AM, Argiriadi MA, Barberis C, Borhani DW, Burchat A, Calderwood DJ, Cunha GA, Dixon RW, Frank KE, Johnson EF, Kamens J, Kwak S, Li B, Mullen KD, Perron DC, Wang L, Wishart N, Wu X, Zhang X, Zmetra TR, Talanian RV. Harris CM, et al. Among authors: johnson ef. Bioorg Med Chem Lett. 2010 Jan 1;20(1):334-7. doi: 10.1016/j.bmcl.2009.10.103. Epub 2009 Oct 29. Bioorg Med Chem Lett. 2010. PMID: 19926477
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: johnson ef. 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
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: johnson ef. 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
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: johnson ef. 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 oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers.
Zhu GD, Gandhi VB, Gong J, Luo Y, Liu X, Shi Y, Guan R, Magnone SR, Klinghofer V, Johnson EF, Bouska J, Shoemaker A, Oleksijew A, Jarvis K, Park C, Jong RD, Oltersdorf T, Li Q, Rosenberg SH, Giranda VL. Zhu GD, et al. Among authors: johnson ef. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3424-9. doi: 10.1016/j.bmcl.2006.04.005. Epub 2006 Apr 27. Bioorg Med Chem Lett. 2006. PMID: 16644221
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. Among authors: johnson ef. 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
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.
Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM. Szczepankiewicz BG, et al. Among authors: johnson ef. J Med Chem. 2006 Jun 15;49(12):3563-80. doi: 10.1021/jm060199b. J Med Chem. 2006. PMID: 16759099
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. Among authors: johnson ef. 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
Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.
Zhao H, Serby MD, Xin Z, Szczepankiewicz BG, Liu M, Kosogof C, Liu B, Nelson LT, Johnson EF, Wang S, Pederson T, Gum RJ, Clampit JE, Haasch DL, Abad-Zapatero C, Fry EH, Rondinone C, Trevillyan JM, Sham HL, Liu G. Zhao H, et al. Among authors: johnson ef. J Med Chem. 2006 Jul 27;49(15):4455-8. doi: 10.1021/jm060465l. J Med Chem. 2006. PMID: 16854050
288 results