| Literature DB >> 16678413 |
Sheela A Thomas1, Tongmei Li, Keith W Woods, Xiaohong Song, Garrick Packard, John P Fischer, Robert B Diebold, Xuesong Liu, Yan Shi, Vered Klinghofer, Eric F Johnson, Jennifer J Bouska, Amanda Olson, Ran Guan, Shayna R Magnone, Kennan Marsh, Yan Luo, Saul H Rosenberg, Vincent L Giranda, Qun Li.
Abstract
Based on lead compounds 2 and 3 a series of 3,5-disubstituted pyridines have been designed and evaluated for inhibition of AKT/PKB. Modifications at the 3 position of the pyridine ring led to a number of potent compounds with improved physical properties, resulting in the identification of 11g as a promising, orally active Akt inhibitor. The synthesis, structure-activity relationship studies, and pharmacokinetic data are presented in this paper.Entities:
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Year: 2006 PMID： 16678413 DOI： 10.1016/j.bmcl.2006.04.046
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823