Synthesis and biological activity of some rigid analogues of flavone-8-acetic acid

Bioorg Med Chem. 2000 Jan;8(1):239-46. doi: 10.1016/s0968-0896(99)00282-5.

Abstract

Some rigid analogues of flavone-8-acetic acid are described. Direct in vitro toxicity of the synthesised compounds was evaluated towards four tumoral cell lines and the ability of these compounds to stimulate mouse peritoneal macrophages in culture to become tumoricidal (indirect toxicity) was also studied. All compounds were able to induce direct cytotoxicity only at very high concentrations but showed a remarkable indirect activity. In particular compound 4d was able to significantly increase macrophage lytic properties and has been selected for further investigations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Division / drug effects
  • Cells, Cultured
  • Flavonoids / chemical synthesis*
  • Flavonoids / pharmacology*
  • Flavonoids / toxicity
  • Humans
  • Macrophages, Peritoneal / drug effects
  • Macrophages, Peritoneal / immunology
  • Magnetic Resonance Spectroscopy
  • Mice
  • Tumor Cells, Cultured

Substances

  • Flavonoids
  • flavone acetic acid