Potent and selective thiophene urea-templated inhibitors of S6K
P Ye, C Kuhn, M Juan, R Sharma, B Connolly… - Bioorganic & medicinal …, 2011 - Elsevier
P Ye, C Kuhn, M Juan, R Sharma, B Connolly, G Alton, H Liu, R Stanton, NM Kablaoui
Bioorganic & medicinal chemistry letters, 2011•ElsevierS6K1 (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.
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.
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.
Elsevier