Synthesis and Cytotoxic Evaluation of Monocarbonyl Analogs of Curcumin as Potential Anti-Tumor Agents

Drug Dev Res. 2016 Feb;77(1):43-9. doi: 10.1002/ddr.21291. Epub 2016 Feb 5.


Preclinical Research A series of mono-carbonyl curcumin analogs with different substituents at the 4/4'-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines using a methyl thiazolyl tetrazolium assay. Several of the curcumin analogs, especially B114, exhibited a wide-spectrum of anti-tumor properties in all tested cell lines, indicating their potential in as anti-cancer lead compounds. Further toxicity testing in the NRK-52E kidney cell line revealed that the analogs A111, A113, and B114 had comparable or higher safety than curcumin. These data suggested that the introduction of appropriate substituents in the 4/4'-positions could be a promising approach for curcumin-based drug design.

Keywords: anti-tumor activity; monocarbonyl curcumin analogs; synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Curcumin / analogs & derivatives*
  • Drug Screening Assays, Antitumor
  • HeLa Cells
  • Hep G2 Cells
  • Humans
  • Molecular Structure


  • Antineoplastic Agents
  • Curcumin