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高等学校化学研究 ›› 2016, Vol. 32 ›› Issue (6): 938-942.doi: 10.1007/s40242-016-6301-5

• Articles • 上一篇    下一篇

Synthesis and Tumor Cytotoxicity of Novel 1, 2, 3-Triazole-substituted 3-Oxo-oleanolic Acid Derivatives

LI Fengran, LIU Yang, WANG Shuai, WEI Gaofei, CHENG Maosheng   

  1. Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China
  • 收稿日期:2016-09-01 修回日期:2016-09-23 出版日期:2016-12-01 发布日期:2016-10-24
  • 通讯作者: LIU Yang, E-mail:y.liu@syphu.edu.cn; CHENG Maosheng, E-mail:mscheng@syphu.edu.cn E-mail:y.liu@syphu.edu.cn;mscheng@syphu.edu.cn
  • 基金资助:

    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).

Synthesis and Tumor Cytotoxicity of Novel 1, 2, 3-Triazole-substituted 3-Oxo-oleanolic Acid Derivatives

LI Fengran, LIU Yang, WANG Shuai, WEI Gaofei, CHENG Maosheng   

  1. Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China
  • Received:2016-09-01 Revised:2016-09-23 Online:2016-12-01 Published:2016-10-24
  • Contact: LIU Yang, E-mail:y.liu@syphu.edu.cn; CHENG Maosheng, E-mail:mscheng@syphu.edu.cn E-mail:y.liu@syphu.edu.cn;mscheng@syphu.edu.cn
  • Supported by:

    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).

摘要：

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).

关键词: 3-Oxo-oleanolic acid, 1,2,3-Triazole, Tumor cytotoxicity

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).

Key words: 3-Oxo-oleanolic acid, 1,2,3-Triazole, Tumor cytotoxicity