Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2485-8. doi: 10.1016/s0960-894x(03)00485-2.


1,5-Diarylbenzimidazoles have been identified as potent inhibitors of KDR kinase activity. The series was developed with a goal of finding compounds with optimal drug-like properties. This communication describes structural modifications in the series that enhance solubility, lower protein binding, and provide compounds with excellent potency and pharmacokinetic profiles.

MeSH terms

  • Animals
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / pharmacology*
  • Chemical Phenomena
  • Chemistry, Physical
  • Dogs
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / pharmacology*
  • Half-Life
  • Hydrogen-Ion Concentration
  • Indicators and Reagents
  • Molecular Conformation
  • Rats
  • Structure-Activity Relationship
  • Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*


  • Benzimidazoles
  • Enzyme Inhibitors
  • Indicators and Reagents
  • Vascular Endothelial Growth Factor Receptor-2