| Literature DB >> 18294842 |
John C Hartnett1, Stanley F Barnett, Mark T Bilodeau, Deborah Defeo-Jones, George D Hartman, Hans E Huber, Raymond E Jones, Astrid M Kral, Ronald G Robinson, Zhicai Wu.
Abstract
This letter shows inhibitor SAR on a pyridine series of allosteric Akt inhibitors to optimize enzymatic and cellular potency. We have optimized 2,3,5-trisubstituted pyridines to give potent Akt1 and Akt2 inhibitors in both enzyme and cell based assays. In addition, we will also highlight the pharmacokinetic profile of an optimized inhibitor that has low clearance and long half-life in dogs.Entities:
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Year: 2007 PMID： 18294842 DOI： 10.1016/j.bmcl.2007.12.040
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823