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

作　　者：LI Fengran LIU Yang WANG Shuai WEI Gaofei CHENG 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》2016年第6期938-942,共5页高等学校化学研究（英文版）

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 

分 类 号：O[理学]