The Preparation Of Methylchalcone Oxime Derivatives And Study On Their Antitumor Activities

Cytochrome P450s were related to various tumorigenesis for its functionas catalysts in the metabolism of endogenous and exogenous compounds.Cytochrome P4501A1(CYP1A1) is closely related to the metabolicactivation of various procarcinogens and premutagens, as well as thedevelopment of tumor. Cytochrome P4501B1(CYP1B1) is regarded tospecifically express in various human cancer cells, and participate in theoxidative metabolism of drugs and activation of prodrugs. CYP1A1andCYP1B1have become new targets for the study of target-oriented antitumorprodrug.In this paper, we summarized the antitumor activity of chalcone analogs,using Cytochrome P4501B1as a target enzyme and methylchalcone oximeas a lead compound, thirty-one novel methylchalcone oxime derivatives were designed and synthesized systematically, including twenty-threemethylchalcone oxime ethers and eight methylchalcone oxime esters. Theirchemical structures were confirmed by1H-NMR and MS, and all thecompounds have not been reported in literatures.The target compounds were evaluated in vitro for their inhibitory effectsagainst the TCDD-induced MCF-7cell lines. Most of compounds displaygood inhibitory effects on the TCDD-induced MCF-7cell lines.The structure-activity relationships of the compounds mentioned abovehave been explored, which may make theoretical and practical bases forfuture work on the project searching for more target-oriented antitumorprodrug.