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

Abstract

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).