Antimitotic and antiproliferative activities of chalcones: forward structure-activity relationship

J Med Chem. 2008 Apr 10;51(7):2307-10. doi: 10.1021/jm0708331. Epub 2008 Feb 23.

Abstract

A series of 59 chalcones was prepared and evaluated for the antimitotic effect against K562 leukemia cells. The most active chalcones were evaluated for their antiproliferative activity against a panel of 11 human and murine cell cancer lines. We found that three chalcones were of great interest as potential antimitotic drugs. In vivo safety studies conducted on one of the most active chalcones revealed that the compound was safe, allowing further in vivo antitumor evaluation.

MeSH terms

  • Animals
  • Antimitotic Agents / chemistry
  • Antimitotic Agents / pharmacology*
  • Antimitotic Agents / toxicity
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / toxicity
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Chalcones / chemistry
  • Chalcones / pharmacology*
  • Chalcones / toxicity
  • Drug Screening Assays, Antitumor
  • Drug-Related Side Effects and Adverse Reactions
  • Humans
  • Mice
  • Molecular Structure
  • Stereoisomerism
  • Structure-Activity Relationship
  • Survival Rate

Substances

  • Antimitotic Agents
  • Antineoplastic Agents
  • Chalcones