Antitumor effects of curcumin and structurally beta-diketone modified analogs on multidrug resistant cancer cells

Manuela Labbozzetta, Natale D'Alessandro, Paola Poma, Monica Notarbartolo Di Villarosa, Michele Rizzi, Paolo Marchetti, Riccardo Baruchello, Riccardo Rondanin, Daniele Simoni, Alessandra Alaimo, Francesco Invidiata, Valeria Carina

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Abstract

Using concepts of bioisostery a series of curcumin analogs were synthesized: the diketonic system of the compound was elaborated into enaminones, oximes, and the isoxazole heterocycle. The cell growth inhibitory and apoptosis inducing effects of the new analogs were evaluated by in vitro assays in the hepatocellular carcinoma HA22T/VGH cells, as well as in the MCF-7 breast cancer cell line and in its multidrug resistant (MDR) variant MCF-7R. Increased antitumor activity on all cell lines was found with the isoxazole analog and especially with the benzyl oxime derivative; in the HA22T/VGH cell model, the latter compound inhibited constitutive NF-kappaB activation
Original languageEnglish
Pages (from-to)845-849
Number of pages5
JournalBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume18
Publication statusPublished - 2008

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All Science Journal Classification (ASJC) codes

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

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