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Bioorg Med Chem Lett. 2008 Mar 15;18(6):2194-7. doi: 10.1016/j.bmcl.2007.12.040. Epub 2007 Dec 23.

Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., PO Box 4, West Point, PA 19486, USA. john_hartnett@merck.com

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.

PMID:
18294842
DOI:
10.1016/j.bmcl.2007.12.040
[Indexed for MEDLINE]

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