期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 8, 页码 2244-2248出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.094
关键词
AKT; Kinase
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 GSK3 beta. (c) 2009 Elsevier Ltd. All rights reserved.
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