2. Academic Validation
  3. Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors

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

  • Bioorg Med Chem Lett. 2012 Aug 1;22(15):5114-7. doi: 10.1016/j.bmcl.2012.05.104.
Kevin K-C Liu 1,  Simon Bailey,  Dac M Dinh,  Hieu Lam,  Chunze Li,  Peter A Wells,  Min-Jean Yin,  Aihua Zou
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Chemistry Department, La Jolla, CA 92120, USA. [email protected]
PMID: 22765900 DOI: 10.1016/j.bmcl.2012.05.104
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-108338
    mTOR Inhibitor