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

Bioorg Med Chem Lett. 2008 Jan 15;18(2):845-9. doi: 10.1016/j.bmcl.2007.11.021.

Daniele Simoni ¹, Michele Rizzi, Riccardo Rondanin, Riccardo Baruchello, Paolo Marchetti, Francesco Paolo Invidiata, Manuela Labbozzetta, Paola Poma, Valeria Carina, Monica Notarbartolo, Alessandra Alaimo, Natale D'Alessandro

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Affiliation

1 Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17/19, 44100 Ferrara, Italy. [email protected]

PMID: 18039573 DOI: 10.1016/j.bmcl.2007.11.021

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.

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