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

Marina Sala, Adele Chimento, Carmela Saturnino, Isabel M. Gomez-Monterrey, Simona Musella, Alessia Bertamino, Ciro Milite, Maria Stefania Sinicropi, Anna Caruso, Rosa Sirianni, Paolo Tortorella, Ettore Novellino, Pietro Campiglia, Vincenzo Pezzi

Research output: Contribution to journalArticle

43 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)4990-4995
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number17
DOIs
StatePublished - Sep 1 2013

Keywords

  • 2,3-Thiazolidin-4-one derivatives
  • Breast cancer cells
  • MCF-7
  • Polyphenol
  • Resveratrol analogs anticancer drugs
  • SKBR3

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Sala, M., Chimento, A., Saturnino, C., Gomez-Monterrey, I. M., Musella, S., Bertamino, A., Milite, C., Sinicropi, M. S., Caruso, A., Sirianni, R., Tortorella, P., Novellino, E., Campiglia, P., & Pezzi, V. (2013). Synthesis and cytotoxic activity evaluation of 2,3-thiazolidin-4-one derivatives on human breast cancer cell lines. Bioorganic and Medicinal Chemistry Letters, 23(17), 4990-4995. https://doi.org/10.1016/j.bmcl.2013.06.051