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

Adele Chimento, 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

Research output: Contribution to journalArticlepeer-review

37 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)6401-6405
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number23
DOIs
StatePublished - Dec 1 2013

Keywords

  • 3-Chloro-azetidin-2-one derivatives
  • Breast cancer
  • MCF-7
  • 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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