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, D., RIZZI, M., RONDANIN, R., BARUCHELLO, R., MARCHETTI, P., INVIDIATA, F., et al. (2008). Antitumor effects of curcumin and structurally beta-diketone modified analogs on multidrug resistant cancer cells. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18(2), 845-849 [10.1016/j.bmcl.2007.11.021].

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

INVIDIATA, Francesco;LABBOZZETTA, Manuela;POMA, Paola;CARINA, Valeria;NOTARBARTOLO DI VILLAROSA, Monica;ALAIMO, Alessandra;D'ALESSANDRO, Natale
2008-01-01

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
2008
Settore BIO/14 - Farmacologia
SIMONI, D., RIZZI, M., RONDANIN, R., BARUCHELLO, R., MARCHETTI, P., INVIDIATA, F., et al. (2008). Antitumor effects of curcumin and structurally beta-diketone modified analogs on multidrug resistant cancer cells. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18(2), 845-849 [10.1016/j.bmcl.2007.11.021].
File in questo prodotto:
File Dimensione Formato  
Simoni.pdf

Solo gestori archvio

Dimensione 234.13 kB
Formato Adobe PDF
234.13 kB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/13316
Citazioni
  • ???jsp.display-item.citation.pmc??? 17
  • Scopus 90
  • ???jsp.display-item.citation.isi??? 75
social impact