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Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors. | LitMetric

Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors.

Bioorg Med Chem Lett

Pfizer Global Research and Development, Chemistry Department, La Jolla, CA 92120, USA.

Published: August 2012

AI Article Synopsis

Article Abstract

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.

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Source
http://dx.doi.org/10.1016/j.bmcl.2012.05.104DOI Listing

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