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Bioorg Med Chem Lett. 2009 Apr 15;19(8):2244-8. doi: 10.1016/j.bmcl.2009.02.094. Epub 2009 Feb 27.

Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.

Author information

1
Oncology Chemistry, GlaxoSmithKline, Collegeville, PA 19426, USA.

Abstract

A pyrrolopyridinyl thiophene carboxamide 7 was discovered as a tractable starting point for a lead optimization effort in an AKT kinase inhibition program. SAR studies aided by a co-crystal structure of 7 in AKT2 led to the identification of AKT inhibitors with subnanomolar potency. Representative compounds showed antiproliferative activity as well as inhibition of phosphorylation of the downstream target GSK3beta.

PMID:
19285393
DOI:
10.1016/j.bmcl.2009.02.094
[Indexed for MEDLINE]

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