Effects of alpha-substitutions on structure and biological activity of anticancer chalcones

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5844-8. doi: 10.1016/j.bmcl.2006.08.065. Epub 2006 Sep 1.

Abstract

Chalcones are known to exhibit antimitotic properties caused by inhibition of tubulin polymerisation. We describe here the effects of different alpha-substitutions, in particular alpha-fluorination, on the structure and biological activity of a series of chalcones.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimitotic Agents / chemical synthesis
  • Antimitotic Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Chalcone / analogs & derivatives
  • Chalcone / chemical synthesis
  • Chalcone / pharmacology*
  • Humans
  • K562 Cells
  • Structure-Activity Relationship
  • Tubulin / metabolism*
  • Tumor Cells, Cultured / drug effects*

Substances

  • Antimitotic Agents
  • Antineoplastic Agents
  • Tubulin
  • Chalcone