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

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...

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Bibliographic Details
Published inChemical research in Chinese universities Vol. 32; no. 6; pp. 938 - 942
Main Authors Li, Fengran, Liu, Yang, Wang, Shuai, Wei, Gaofei, Cheng, Maosheng
Format Journal Article
LanguageEnglish
Published Changchun Jilin University and The Editorial Department of Chemical Research in Chinese Universities 01.12.2016
Springer Nature B.V
Subjects
Analytical Chemistry
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
Inorganic Chemistry
Organic Chemistry
Physical Chemistry
Triazoles
3-Oxo-oleanolic acid
Tumor cytotoxicity
1,2,3-Triazole
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Summary: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 6 c, with a p -NO 2 at the bezene ring, possesses the best inhibitory activity against A375-S2(IC 50 =2.82 μmol/L) and HT1080(IC 50 =1.69 μmol/L).
ISSN:1005-9040
2210-3171
DOI:10.1007/s40242-016-6301-5