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Synthesis and cytotoxic activity evaluation of 2,3-thiazolidin-4-one derivatives on human breast cancer cell lines
Authors: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
Affiliation:1. Department of Pharmaceutical Science, Division of Biomedicine, University of Salerno, Fisciano, SA 84084, Italy;2. Department of Pharmacy, Health and Nutrition Sciences, University of Calabria, Arcavacata di Rende, Cosenza 87036, Italy;3. Department of Pharmaceutical and Toxicological Chemistry, University of Naples “Federico II”, Naples 8013, Italy;4. Department Pharmaco-Biological, University of Messina, 98168 Messina, Italy;5. Department Pharmaceutical Chemistry, University of Bari “Aldo Moro”, 70125 Bari, Italy
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:Resveratrol analogs anticancer drugs  2,3-Thiazolidin-4-one derivatives  Polyphenol  Breast cancer cells  MCF-7  SKBR3
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