Search results for "Diketone modified analog"

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Lack of nucleophilic addition in the isoxazole and pyrazole diketone modified analogs of curcumin; implications for their antitumor and chemosensitiz…

2009

Curcumin (CUR) can be considered as a good lead compound for the design of new anticancer drugs. Further, structure-activity relationship studies may clarify the importance of the redox activities in the antitumor effects of the drug. We have elaborated the alpha,beta-unsaturated 1,3-diketone moiety of CUR into the isoxazole (ISO) and pyrazole (PYR) derivatives. These derivatives should be much less prone to nucleophilic addition than CUR and benzyl mercaptan addition analyses showed that indeed they do not form isolable conjugated products. When compared with CUR, ISO and PYR exhibited increased cell growth inhibitory and pro-apoptotic effects in liver cancer HA22T/VGH cells as well as in …

CurcuminMagnetic Resonance SpectroscopyStereochemistryDiketone modified analogAntineoplastic AgentsPyrazoleToxicologyChemosensitizationCell Linechemistry.chemical_compoundStructure-Activity RelationshipSettore BIO/10 - BiochimicaCell Line TumorStructure–activity relationshipHumansButhionine sulfoximineIsoxazoleButhionine SulfoximineChromatography High Pressure LiquidDiketoneChromatographyTumorCell growthGeneral MedicineGlutathioneIsoxazolesFlow CytometrySettore CHIM/08 - Chimica FarmaceuticaAcetylcysteine; Antineoplastic Agents; Buthionine Sulfoximine; Cell Line; Tumor; Chromatography; High Pressure Liquid; Curcumin; Flow Cytometry; Humans; Isoxazoles; Magnetic Resonance Spectroscopy; Pyrazoles; Structure-Activity RelationshipAcetylcysteinechemistryHigh Pressure LiquidCurcuminSettore BIO/14 - FarmacologiaPyrazolesNucleophilic additionAntitumor activityChemico-biological interactions
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