Title of article
Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors
Author/Authors
John C. Hartnett، نويسنده , , Stanley F. Barnett، نويسنده , , Mark T. Bilodeau، نويسنده , , Deborah Defeo-Jones، نويسنده , , George D. Hartman، نويسنده , , Hans E. Huber، نويسنده , , Raymond E. Jones، نويسنده , , Astrid M. Kral، نويسنده , , Ronald G. Robinson، نويسنده , , Zhicai Wu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
2194
To page
2197
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.
Keywords
enzymatic , AKT2 , Inhibitors , cellular , AKT1
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799323
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