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

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 exa...

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Hauptverfasser: Wei, Gaofei, Luan, Weijing, Wang, Shuai, Cui, Shanshan, Li, Fengran, Liu, Yongxiang, Liu, Yang, Cheng, Maosheng
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Sprache:eng
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Zusammenfassung: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.
ISSN:1477-0520
1477-0539
DOI:10.1039/c4ob01605j