Synthesis of curcumin mimics with multidrug resistance reversal activities

Bioorg Med Chem. 2008 Apr 1;16(7):3608-15. doi: 10.1016/j.bmc.2008.02.012. Epub 2008 Feb 8.

Abstract

In order to discover novel multidrug resistance (MDR) reversal agents for efficient cancer chemotherapy, the unsymmetrical curcumin mimics with various amide moieties (6-19) were synthesized and evaluated their MDR reversal activities in MDR cell line KBV20C. Among the tested compounds, 13, 16, and 17 showed potent MDR reversal activities by inhibiting drug efflux function of P-glycoprotein in KB20C cells, and almost recovered the cytotoxicity of vincristine and paclitaxel against KBV20C cell to the degree of potency against drug sensitive KB cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cross-Linking Reagents / chemistry
  • Curcumin / analogs & derivatives*
  • Curcumin / chemical synthesis
  • Curcumin / chemistry
  • Curcumin / pharmacology*
  • Drug Resistance, Multiple / drug effects*
  • Drug Resistance, Neoplasm / drug effects
  • Humans
  • Molecular Structure
  • Stereoisomerism

Substances

  • Cross-Linking Reagents
  • Curcumin