Synthesis and tumor cytotoxicity of novel 1,2,3-triazole-substituted 3-oxo-oleanolic acid derivatives

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• 作者：Fengran Li ; Yang Liu ; Shuai Wang ; Gaofei Wei…
• 关键词：3 ; Oxo ; oleanolic acid ; 1 ; 2 ; 3 ; Triazole ; Tumor cytotoxicity
• 刊名：Chemical Research in Chinese Universities
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：32
• 期：6
• 页码：938-942
• 全文大小：
• 刊物主题：Chemistry/Food Science, general; Analytical Chemistry; Inorganic Chemistry; Organic Chemistry; Physical Chemistry;
• 出版者：Jilin University and The Editorial Department of Chemical Research in Chinese Universities
• ISSN：2210-3171
• 卷排序：32

文摘

Fifteen novel 3-oxo-oleanolic acid esters bearing aryl substituted 1,2,3-triazolyl methyl moiety were synthesized via the method of Copper(I)-catalyzed Huisgen cycloaddition. The cytotoxicity evaluation results of these compounds against five human tumor cell lines show that most of these compounds presented potent activity and selectivity against A375-S2 and HT1080 cells. Compound 6c, with a p-NO₂ at the bezene ring, possesses the best inhibitory activity against A375-S2(IC₅₀=2.82 μmol/L) and HT1080(IC₅₀=1.69 μmol/L).