Broad spectrum alkynyl inhibitors of T315I Bcr-Abl

  • Bioorg Med Chem Lett. 2010 Jul 15;20(14):4196-200. doi: 10.1016/j.bmcl.2010.05.043.
Xianming Deng  1 ,  Sang Min Lim ,  Jianming Zhang ,  Nathanael S Gray
Affiliations
  • 1. Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, United States.
PMID: 20541934 DOI: 10.1016/j.bmcl.2010.05.043
Abstract

A series of alkyne-containing type II inhibitors with potent inhibitory activity of T315I Bcr-Abl has been identified. The most active compound 4 exhibits an EC(50) of less than 1 nM against wild-type Bcr-Abl and an EC(50) of 10 nM against T315I mutant but is broadly active against a number of Other kinases.