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HERO ID
7112710
Reference Type
Journal Article
Title
Potent and selective thiophene urea-templated inhibitors of S6K
Author(s)
Ye, P; Kuhn, C; Juan, M; Sharma, R; Connolly, B; Alton, G; Liu, Hu; Stanton, R; Kablaoui, NM; ,
Year
2011
Is Peer Reviewed?
Yes
Journal
Bioorganic & Medicinal Chemistry Letters
ISSN:
0960-894X
EISSN:
1464-3405
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Location
OXFORD
Volume
21
Issue
2
Page Numbers
849-852
Language
English
PMID
21185721
DOI
10.1016/j.bmcl.2010.11.069
Web of Science Id
WOS:000285998000050
Abstract
S6K1 (p70 S6 kinase-1) is thought to play a critical role in the development of obesity and insulin resistance, thus making it an attractive target in developing medicines for the treatment of these disorders. We describe a novel thiophene urea class of S6K inhibitors. The lead matter for the development of these inhibitors came from mining the literature for reports of weak off-target S6K activity. These optimized inhibitors exhibit good potency and excellent selectivity for S6K over a panel of 43 kinases. (C) 2010 Elsevier Ltd. All rights reserved.
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