Design and synthesis of novel iminothiazinylbutadienols and divinylpyrimidinethiones as ARE inducers

新型亚氨基噻嗪基丁二烯醇和二乙烯基嘧啶硫酮作为ARE诱导剂的设计与合成

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Abstract

Novel iminothiazinylbutadienols and divinylpyrimidinethiones were designed and synthesized as analogues of curcumin with its diketone moiety masked as a heterocyclic adduct with thiourea. The chemical stability of these novel heterocyclic compounds was improved as compared to curcumin. They exhibit longer half-lives and do not react with nucleophilic thiols under physiological conditions. In an ARE-luciferase reporter assay, some of these new curcumin analogues are more effective ARE activators than curcumin and isothiocyanates.

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