6533b85cfe1ef96bd12bc9ed

RESEARCH PRODUCT

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

Alessandra AlaimoMonica NotarbartoloManuela LabbozzettaRiccardo BaruchelloPaola PomaRiccardo RondaninMichele RizziValeria CarinaPaolo MarchettiDaniele SimoniNatale D'alessandroFrancesco Paolo Invidiata

subject

Cell growth inhibitionSpectrometry Mass Electrospray IonizationCurcuminMagnetic Resonance SpectroscopyMDR breast cancer cellsClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsBiochemistrychemistry.chemical_compoundCell Line TumorDrug DiscoveryNF-κB inhibitionHumansIsoxazoleCytotoxicityMolecular BiologyChromatography High Pressure LiquidCell growthOrganic ChemistryCell growth inhibition; Curcumin oxime derivatives; MDR breast cancer cells; NF-κB inhibition;KetonesCurcumin oxime derivativesDrug Resistance MultipleMultiple drug resistancechemistryBiochemistryDrug Resistance NeoplasmCell cultureApoptosisCancer cellSettore BIO/14 - FarmacologiaCurcuminMolecular MedicineCell

description

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-κB activation.

yearjournalcountryeditionlanguage
2007-09-18Bioorganic & Medicinal Chemistry Letters
https://doi.org/10.1016/j.bmcl.2007.11.021