Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3405-9. doi: 10.1016/j.bmcl.2009.05.040. Epub 2009 May 18.

Abstract

Substituted benzimidazoles were profiled as inhibitors of kinesin spindle protein (KSP), an increasingly important target for the development of anticancer drugs. This series demonstrated the monoastral phenotypic response and was found to be active in both enzymatic and cellular-based assays.

MeSH terms

  • Animals
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology
  • Caco-2 Cells
  • Cell Line
  • Cytochrome P-450 Enzyme System / metabolism
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Kinesins / antagonists & inhibitors*
  • Kinesins / metabolism
  • Rats
  • Structure-Activity Relationship

Substances

  • Benzimidazoles
  • Enzyme Inhibitors
  • KIF11 protein, human
  • Cytochrome P-450 Enzyme System
  • benzimidazole
  • Kinesins