Synthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4044-8. doi: 10.1016/j.bmcl.2012.04.083. Epub 2012 Apr 25.

Abstract

A series of hydroxybenzoxazole derivatives was synthesized, and their c-Met kinase inhibitory activity was evaluated. Described herein is a potent c-Met inhibitor by structural modification of the parent benzoxazole scaffold, with particular focus on the hydroxyl substituent of the benzoxazole moiety.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminopyridines / chemical synthesis*
  • Aminopyridines / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Benzoxazoles / chemical synthesis*
  • Benzoxazoles / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Computer Simulation
  • Humans
  • Models, Molecular
  • Proto-Oncogene Proteins c-met / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-met / chemistry
  • Structure-Activity Relationship
  • fms-Like Tyrosine Kinase 3 / antagonists & inhibitors*
  • fms-Like Tyrosine Kinase 3 / chemistry

Substances

  • Aminopyridines
  • Antineoplastic Agents
  • Benzoxazoles
  • FLT3 protein, human
  • Proto-Oncogene Proteins c-met
  • fms-Like Tyrosine Kinase 3