1.
Bioorg Med Chem Lett
; 21(2): 849-52, 2011 Jan 15.
Article
in English
| MEDLINE
| ID: mdl-21185721
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.