Synthesis and Anticancer Activities of Glycyrrhetinic Acid Derivatives

Molecules. 2016 Feb 6;21(2):199. doi: 10.3390/molecules21020199.

Abstract

A total of forty novel glycyrrhetinic acid (GA) derivatives were designed and synthesized. The cytotoxic activity of the novel compounds was tested against two human breast cancer cell lines (MCF-7, MDA-MB-231) in vitro by the MTT method. The evaluation results revealed that, in comparison with GA, compound 42 shows the most promising anticancer activity (IC50 1.88 ± 0.20 and 1.37 ± 0.18 µM for MCF-7 and MDA-MB-231, respectively) and merits further exploration as a new anticancer agent.

Keywords: MCF-7; MDA-MB-231; anticancer; derivatives; glycyrrhetinic acid (GA).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Survival / drug effects
  • Doxorubicin / pharmacology
  • Drug Screening Assays, Antitumor
  • Glycyrrhetinic Acid / analogs & derivatives*
  • Glycyrrhetinic Acid / chemical synthesis*
  • Glycyrrhetinic Acid / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • MCF-7 Cells

Substances

  • Antineoplastic Agents
  • Doxorubicin
  • Glycyrrhetinic Acid