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

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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).

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Correspondence to Yang Liu or Maosheng Cheng.

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Supported by the National Natural Science Foundation of China(Nos.81473087, 81273358, 30772641) and the Program for Liaoning Excellent Talents in University, China(No.LJQ2014110).

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Li, F., Liu, Y., Wang, S. et al. Synthesis and tumor cytotoxicity of novel 1,2,3-triazole-substituted 3-oxo-oleanolic acid derivatives. Chem. Res. Chin. Univ. 32, 938–942 (2016). https://doi.org/10.1007/s40242-016-6301-5

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  • DOI: https://doi.org/10.1007/s40242-016-6301-5

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