Article ID Journal Published Year Pages File Type
1376859 Bioorganic & Medicinal Chemistry Letters 2008 4 Pages PDF
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.

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Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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