Developments in the anticancer activity of structurally modified curcumin: An up-to-date review

Eur J Med Chem. 2019 Sep 1:177:76-104. doi: 10.1016/j.ejmech.2019.04.058. Epub 2019 May 14.

Abstract

Curcumin is a pharmacologically active polyphenol derived from the popular spice element-Turmeric. The therapeutic activity of curcumin has been extensively investigated over the last few decades and reports suggest the role of curcumin in a large number of biological activities, particularly its prominent anticancer activity. Curcumin, being a pleiotropic molecule, is a regulator of multiple molecular targets which play crucial roles in various cell signaling pathways. It is known to suppress transformation, inhibit proliferation as well as induce apoptosis. However, despite all these benefits, the efficacy of curcumin remains limited due to its poor bioavailability, poor absorption within the systemic circulation and rapid elimination from the body. To overcome these limiting factors, researchers all around the world are working towards designing a synthetic and superior curcuminoid by making suitable structural modifications to the parent skeleton. These curcuminoids, mainly analogues and derivatives, will not only improve the physicochemical properties but also enhance the efficacy simultaneously. The present review will provide a comprehensive account of the analogues and derivatives of curcumin that have been reported since 2014 which have indicated a better anticancer activity than curcumin.

Keywords: Analogue; Anticancer; Curcumin; Derivative; Structural modification.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Curcumin / analogs & derivatives*
  • Curcumin / chemical synthesis
  • Curcumin / pharmacology*
  • Humans
  • Molecular Structure

Substances

  • Antineoplastic Agents
  • Curcumin