Design, synthesis, and cytostatic activity of novel cyclic curcumin analogues

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5624-9. doi: 10.1016/j.bmcl.2007.07.079. Epub 2007 Aug 22.

Abstract

A series of novel cyclic analogues of curcumin were synthesized and analyzed for in vitro cytostatic activity. Condensation of 2-acetylcycloalkanones with a variety of aromatic aldehydes resulted in the formation of 2-arylidene-6-(3-arylacryoyl)-cycloalkanone derivatives. A number of these analogues were found to have significant anticancer activity against representative murine and human cancer cell lines during in vitro bioassays. This corroborated with in vitro cytostatic activity against a panel of 60 cell lines studied at the National Cancer Institute (USA).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Chemical Phenomena
  • Chemistry, Physical
  • Crystallography, X-Ray
  • Curcumin / analogs & derivatives
  • Curcumin / chemical synthesis
  • Curcumin / chemistry*
  • Curcumin / toxicity*
  • Cytostatic Agents / chemical synthesis
  • Cytostatic Agents / chemistry
  • Cytostatic Agents / pharmacology
  • Cytostatic Agents / toxicity*
  • Drug Design*
  • Humans
  • Mice
  • Models, Molecular
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Cytostatic Agents
  • Curcumin