Development of 'DFG-out' inhibitors of gatekeeper mutant kinases

Hwan Geun Choi, Jianming Zhang, Ellen Weisberg, James D. Griffin, Taebo Sim, Nathanael S. Gray

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)


HG-7-85-01(22) and HG-7-86-01(26) are thiazolo[5,4-b]pyridine containing type II tyrosine kinase inhibitors with potent cellular activity against both wild-type and 'gatekeeper' mutant T315I- Bcr-Abl. Here we report on the 'hybrid design' concept and subsequent structure activity guided optimization efforts that resulted in the development of these inhibitors.

Original languageEnglish
Pages (from-to)5297-5302
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number16
Publication statusPublished - 2012 Aug 15


  • Gatekeeper mutant
  • Kinase inhibitor
  • T315I Bcr-Abl
  • Thiazolo[5,4-b]pyridine
  • Type II inhibitor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


Dive into the research topics of 'Development of 'DFG-out' inhibitors of gatekeeper mutant kinases'. Together they form a unique fingerprint.

Cite this