Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development

J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r.

Abstract

This report describes the biological activity, characterization, and SAR leading to 9d (BMS-754807) a small molecule IGF-1R kinase inhibitor in clinical development.

MeSH terms

  • Animals
  • Biomedical Research*
  • Dogs
  • Drug Discovery
  • Humans
  • Mice
  • Models, Molecular
  • Molecular Conformation
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacokinetics
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacokinetics
  • Pyrazoles / pharmacology*
  • Pyrazoles / therapeutic use
  • Rats
  • Receptor, IGF Type 1 / antagonists & inhibitors*
  • Receptor, IGF Type 1 / chemistry
  • Structure-Activity Relationship
  • Triazines / chemistry
  • Triazines / pharmacokinetics
  • Triazines / pharmacology*
  • Triazines / therapeutic use

Substances

  • BMS 754807
  • Protein Kinase Inhibitors
  • Pyrazoles
  • Triazines
  • Receptor, IGF Type 1