1393712-18-9Relevant articles and documents
Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors
Liu, Kevin K.-C.,Bailey, Simon,Dinh, Dac M.,Lam, Hieu,Li, Chunze,Wells, Peter A.,Yin, Min-Jean,Zou, Aihua
, p. 5114 - 5117 (2012)
Novel conformationally-restricted mTOR kinase inhibitors with cyclic sulfone scaffold were designed. Synthesis and structure-activity relationship (SAR) studies are described with emphasis on optimization of the mTOR potency and selectivity against class I PI3Kα kinase. PF-05139962 was identified with excellent mTOR biochemical inhibition, cellular potency, kinase selectivity and in vitro ADME properties.