Chalcones: a new class of antimitotic agents

J Med Chem. 1990 Jul;33(7):1948-54. doi: 10.1021/jm00169a021.

Abstract

A series of chalcones was evaluated as antimitotic agents. One of these, (E)-1-(2,5-dimethoxyphenyl)-3-[4-(dimethylamino)phenyl]-2-methyl-2-pr open- 1-one) (73), was found to be an effective antimitotic agent at a concentration of 4 nM in an in vitro HeLa cell test system. When evaluated in experimental tumor models in vivo, this compound exhibited antitumor activity against L1210 leukemia and B16 melanoma.

Publication types

  • Comparative Study

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Cell Cycle / drug effects
  • Chalcone / analogs & derivatives
  • Chalcone / chemical synthesis*
  • Chalcone / pharmacology
  • HeLa Cells / cytology
  • HeLa Cells / drug effects
  • Humans
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Mitosis / drug effects
  • Molecular Structure
  • Propiophenones / chemical synthesis*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Indicators and Reagents
  • Propiophenones
  • MDL 27048
  • Chalcone