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

41 Citations (Scopus)

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

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Cells
Breast Neoplasms
Derivatives
Cell Line
Biological Availability
Cell growth
Rigidity
Libraries
Growth
resveratrol
Neoplasms

Keywords

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

ASJC Scopus subject areas

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

Cite this

Sala, M., Chimento, A., Saturnino, C., Gomez-Monterrey, I. M., Musella, S., Bertamino, A., ... 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

Synthesis and cytotoxic activity evaluation of 2,3-thiazolidin-4-one derivatives on human breast cancer cell lines. / Sala, Marina; Chimento, Adele; Saturnino, Carmela; Gomez-Monterrey, Isabel M.; Musella, Simona; Bertamino, Alessia; Milite, Ciro; Sinicropi, Maria Stefania; Caruso, Anna; Sirianni, Rosa; Tortorella, Paolo; Novellino, Ettore; Campiglia, Pietro; Pezzi, Vincenzo.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 17, 01.09.2013, p. 4990-4995.

Research output: Contribution to journalArticle

Sala, M, Chimento, A, Saturnino, C, Gomez-Monterrey, IM, Musella, S, Bertamino, A, Milite, C, Sinicropi, MS, 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, vol. 23, no. 17, pp. 4990-4995. https://doi.org/10.1016/j.bmcl.2013.06.051
Sala, Marina ; Chimento, Adele ; Saturnino, Carmela ; Gomez-Monterrey, Isabel M. ; Musella, Simona ; Bertamino, Alessia ; Milite, Ciro ; Sinicropi, Maria Stefania ; Caruso, Anna ; Sirianni, Rosa ; Tortorella, Paolo ; Novellino, Ettore ; Campiglia, Pietro ; Pezzi, Vincenzo. / Synthesis and cytotoxic activity evaluation of 2,3-thiazolidin-4-one derivatives on human breast cancer cell lines. In: Bioorganic and Medicinal Chemistry Letters. 2013 ; Vol. 23, No. 17. pp. 4990-4995.
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