Biological activity of 3-chloro-azetidin-2-one derivatives having interesting antiproliferative activity on human breast cancer cell lines

  • Bioorg Med Chem Lett. 2013 Dec 1;23(23):6401-5. doi: 10.1016/j.bmcl.2013.09.054.
Adele Chimento  1 ,  Marina Sala ,  Isabel M Gomez-Monterrey ,  Simona Musella ,  Alessia Bertamino ,  Anna Caruso ,  Maria Stefania Sinicropi ,  Rosa Sirianni ,  Francesco Puoci ,  Ortensia Ilaria Parisi ,  Carmela Campana ,  Emilia Martire ,  Ettore Novellino ,  Carmela Saturnino ,  Pietro Campiglia ,  Vincenzo Pezzi
Affiliations
  • 1. Department of Pharmacy, Health and Nutrition Sciences, University of Calabria, 87036 Arcavacata di Rende, Cosenza, Italy.
Abstract

Resveratrol (3,4',5 tri-hydroxystilbene), a natural plant polyphenol, has gained interest as a non-toxic agent capable of inducing tumor cell death in a variety of Cancer types. However, therapeutic application of these beneficial effects remains very limited due to its short biological half-life, labile properties, rapid metabolism and elimination. Different studies were undertaken to obtain synthetic analogs of resveratrol with major bioavailability and Anticancer activity. We have synthesized a series 3-chloro-azetidin-2-one derivatives, in which an azetidinone nucleus connects two aromatic rings. Aim of the present study was to investigate the effects of these new 3-chloro-azetidin-2-one resveratrol derivatives on human Breast Cancer cell lines proliferation. Our results indicate that some azetidin-based resveratrol derivatives may become new potent alternative tools for the treatment of human Breast Cancer.

Keywords
3-Chloro-azetidin-2-one derivatives; Breast cancer; MCF-7; Resveratrol analogs anticancer drugs; SKBR3.