Synthetic and biological activity evaluation studies on novel 1,3-diarylpropenones

Bioorg Med Chem. 2001 Feb;9(2):337-45. doi: 10.1016/s0968-0896(00)00249-2.

Abstract

Fourteen novel C-prenylated and O-allylated 1,3-diarylpropenones (chalcones) were synthesized by Claisen-Schmidt condensation reaction of C-prenylated/O-allylated acetophenones with appropriate aldehydes; twelve of these model chalcones were screened in an assay based on the confrontation of invasive human MCF-7/6 mammary carcinoma cells with fragments of normal embryonic chick heart in vitro. Out of the twelve chalcones tested, three were found to exhibit potent anti-invasive activity. Some of these chalcones and their precursor acetophenones were also tested for inhibition of initiation of lipid peroxidation in rat liver microsomes; a prenylated acetophenone carrying two methoxy groups and two free phenolic hydroxy functions was found to be a potential antioxidant.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetophenones / pharmacology
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Antioxidants / chemical synthesis
  • Antioxidants / pharmacology
  • Breast Neoplasms / pathology
  • Chalcone / chemical synthesis
  • Chalcone / pharmacology*
  • Chick Embryo
  • Coculture Techniques
  • Combinatorial Chemistry Techniques
  • Drug Evaluation, Preclinical
  • Female
  • Humans
  • Lipid Peroxidation / drug effects
  • Microsomes, Liver / drug effects
  • Microsomes, Liver / metabolism
  • Myocardium / cytology
  • Neoplasm Invasiveness / prevention & control*
  • Rats
  • Structure-Activity Relationship
  • Tumor Cells, Cultured / drug effects

Substances

  • Acetophenones
  • Antineoplastic Agents
  • Antioxidants
  • Chalcone