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. Epub 2010 May 19.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Alkynes / chemistry
  • Alkynes / pharmacology*
  • Benzamides / chemistry
  • Benzamides / pharmacology*
  • Fusion Proteins, bcr-abl / antagonists & inhibitors*
  • Pyridines / chemistry
  • Pyridines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Alkynes
  • Benzamides
  • HG-6-63-01
  • Pyridines
  • Fusion Proteins, bcr-abl