Synthesis and Tumor Cytotoxicity of Novel1,2,3-Triazole-substituted 3-Oxo-oleanolic Acid Derivatives

查看全文 作　　者：LI [1]Fengran;LIU [1]Yang;WANG [1]Shuai;WEI [1]Gaofei;CHENG [1]Maosheng

机构地区：[1]Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang'110016, P. R. China

出　　处：《Chemical Research in Chinese Universities》索引2016年第32卷第6期,共5页

摘　　要：Fifteen novel 3-oxo-oleanolic acid esters bearing aryl substituted 1,2,3-triazolyl methyl moiety weresynthesized via the method of Copper(I)-catalyzed Huisgen cycloaddifion. The cytotoxicity evaluation results of thesecompounds against five human tumor cell lines show that most of these compounds presented potent activity andselectivity against A375-S2 and HT1080 cells. Compound 6c, with a p-NO2 at the bezene ring, possesses the bestinhibitory activity against A375-S2(IC50=2.82 μmol/L) and HT1080(IC50=1.69 μmol/L). 关键词：3-Oxo-oleanolic acid 1,2,3-TRIAZOLE Tumor CYTOTOXICITY

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Synthesis and Tumor Cytotoxicity of Novel1,2,3-Triazole-substituted 3-Oxo-oleanolic Acid Derivatives

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