Synthesis and cytotoxic activity evaluation of 2,3-thiazolidin-4-one derivatives on human breast cancer cell lines

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4990-5. doi: 10.1016/j.bmcl.2013.06.051. Epub 2013 Jun 26.

Abstract

It is well known that resveratrol (RSV) displayed cancer-preventing and anticancer properties but its clinical application is limited because of a low bioavailability and a rapid clearance from the circulation. Aim of this work was to synthesize pharmacologically active resveratrol analogs with an enhanced structural rigidity and bioavailability. In particular, we have synthesized a library of 2,3-thiazolidin-4-one derivatives in which a thiazolidinone nucleus connects two aromatic rings. Some of these compounds showed strong inhibitory effects on breast cancer cell growth. Our results indicate that some of thiazolidin-based resveratrol derivatives may become a new potent alternative tool for the treatment of human breast cancer.

Keywords: 2,3-Thiazolidin-4-one derivatives; Breast cancer cells; MCF-7; Polyphenol; Resveratrol analogs anticancer drugs; SKBR3.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemical synthesis
  • Antineoplastic Agents, Phytogenic / chemistry*
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Breast Neoplasms / drug therapy*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Resveratrol
  • Stilbenes / chemical synthesis
  • Stilbenes / chemistry*
  • Stilbenes / pharmacology*
  • Thiazolidinediones / chemical synthesis
  • Thiazolidinediones / chemistry*
  • Thiazolidinediones / pharmacology*

Substances

  • Antineoplastic Agents, Phytogenic
  • Stilbenes
  • Thiazolidinediones
  • Resveratrol