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7112710 
Journal Article 
Potent and selective thiophene urea-templated inhibitors of S6K 
Ye, P; Kuhn, C; Juan, M; Sharma, R; Connolly, B; Alton, G; Liu, Hu; Stanton, R; Kablaoui, NM; , 
2011 
Yes 
Bioorganic & Medicinal Chemistry Letters
ISSN: 0960-894X
EISSN: 1464-3405 
PERGAMON-ELSEVIER SCIENCE LTD 
OXFORD 
21 
849-852 
English 
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.