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Bioorg Med Chem Lett. 2010 Jan 15;20(2):673-8. doi: 10.1016/j.bmcl.2009.11.064. Epub 2009 Nov 20.

2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.

Author information

1
Oncology Medicinal Chemistry, GlaxoSmithKline, 1250 S. Collegeville, Rd., Collegeville, PA 19426, United States. hong.2.lin@gsk.com

Abstract

2,3,5-Trisubstituted pyridines have been designed as potent AKT inhibitors that are selective against ROCK1 based on the comparison between AKT and ROCK1 structures. Substitution at the 2-position of the core pyridine is the key element to provide selectivity against ROCK1. An X-ray co-crystal structure of 9p in PKA supports the proposed rationale of ROCK1 selectivity.

PMID:
20006497
DOI:
10.1016/j.bmcl.2009.11.064
[Indexed for MEDLINE]

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