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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Liu KK,Bailey S,Dinh DM,Lam H,Li C,Wells PA,Yin MJ,Zou A

doi

10.1016/j.bmcl.2012.05.104

subject

Has Abstract

pub_date

2012-08-01 00:00:00

pages

5114-7

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00716-0

journal_volume

22

pub_type

杂志文章

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