2. Academic Validation
  3. Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors

Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors

  • Bioorg Med Chem Lett. 2009 Dec 1;19(23):6519-23. doi: 10.1016/j.bmcl.2009.10.049.
Dan M Berger 1,  Nancy Torres,  Minu Dutia,  Dennis Powell,  Greg Ciszewski,  Ariamala Gopalsamy,  Jeremy I Levin,  Kyung-Hee Kim,  Weixin Xu,  James Wilhelm,  YongBo Hu,  Karen Collins,  Larry Feldberg,  Steven Kim,  Eileen Frommer,  Donald Wojciechowicz,  Robert Mallon
Affiliations

Affiliation

  • 1 Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA. bergerd@wyeth.com
PMID: 19864136 DOI: 10.1016/j.bmcl.2009.10.049
Abstract

As part of our research effort to discover B-Raf kinase inhibitors, we prepared a series of C-3 substituted N-(3-(pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamides. X-ray crystallography studies revealed that one of the more potent inhibitors (10n) bound to B-Raf kinase without forming a hinge-binding hydrogen bond. With basic amine residues appended to C-3 aryl residues, cellular activity and solubility were enhanced over previously described compounds of this class.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-18227
    98.66%, Raf抑制剂
    Raf
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