A library of 1,2,3-triazole-substituted oleanolic acid derivatives as anticancer agents: design, synthesis, and biological evaluationElectronic supplementary information (ESI) available. See DOI: 10.1039/c4ob01605j

• Main Authors: Wei, Gaofei, Luan, Weijing, Wang, Shuai, Cui, Shanshan, Li, Fengran, Liu, Yongxiang, Liu, Yang, Cheng, Maosheng
• Format: Journal Article
• Language: English
• Published: 21.01.2015
• ISSN: 1477-0520; 1477-0539
• DOI: 10.1039/c4ob01605j

A series of novel oleanolic acid coupled 1,2,3-triazole derivatives have been designed and synthesized by employing a Cu( i ) catalyzed Huisgen 1,3-dipolar cycloaddition reaction. The anti-proliferative evaluation indicated that some compounds exhibited excellent anti-cancer activity against the examined cancer cell lines. Among all derivatives, compound 3t possesses the best inhibitory activity against HT1080 cells. A series of pharmacology experiments show that compound 3t significantly induced HT1080 cell apoptosis. Therefore, this compound can serve as a promising lead candidate for further study. A series of novel oleanolic acid coupled 1,2,3-triazole derivatives have been designed and synthesized by employing a Cu( i ) catalyzed Huisgen 1,3-dipolar cycloaddition reaction.