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.

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

SIMONI, Daniele;RIZZI, Michele;RONDANIN, Riccardo;BARUCHELLO, Riccardo;MARCHETTI, Paolo;
2008

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.
Simoni, Daniele; Rizzi, Michele; Rondanin, Riccardo; Baruchello, Riccardo; Marchetti, Paolo; Francesco Paolo, Invidiata; Manuela, Labbozzetta; Paola, Poma; Valeria, Carina; Monica, Notarbartolo; Alessandra, Alaimo; Natale, D'Alessandro
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/520839
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