Synthesis and biological evaluation of imidazol-2-one derivatives as potential antitumor agents

Bioorg Med Chem. 2008 Mar 1;16(5):2550-7. doi: 10.1016/j.bmc.2007.11.048. Epub 2007 Nov 22.

Abstract

A new series of aryl substituted imidazol-2-one derivatives structurally related to combretastatin A-4 (CA-4) were synthesized and evaluated for their cytotoxic activities in vitro against various human cancer cell lines including MDR cell line. The cytotoxic effects of compounds 7b and 7i proved to be similar to or greater than that of docetaxel. The highly active compound 7b also exhibited excellent inhibitory activity on tumor growth in vivo.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Imidazoles / chemical synthesis*
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Imidazoles / therapeutic use
  • Mice
  • Molecular Structure
  • Neoplasm Transplantation
  • Neoplasms / drug therapy
  • Neoplasms / pathology
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Imidazoles
  • imidazole