| Literature DB >> 19285393 |
Mark A Seefeld1, Meagan B Rouse, Kenneth C McNulty, Lihui Sun, Jizhou Wang, Dennis S Yamashita, Juan I Luengo, Shuyun Zhang, Elisabeth A Minthorn, Nestor O Concha, Dirk A Heerding.
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.Entities:
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Year: 2009 PMID： 19285393 DOI： 10.1016/j.bmcl.2009.02.094
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823