Synthesis and in vitro antitumor activities of lupeol dicarboxylic acid monoester derivatives

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• 作者：Weijie Li (1)
  Jing Hao (2)
  Yeyu Xiao (3)
  
• 关键词：Lupeol derivative ; Synthesis ; Antitumor activity
• 刊名：Archives of Pharmacal Research
• 出版年：2013
• 出版时间：December 2013
• 年：2013
• 卷：36
• 期：12
• 页码：1447-1453
• 全文大小：
• 作者单位：Weijie Li (1)
  Jing Hao (2)
  Yeyu Xiao (3)
  
  1. Department of Chemistry, Hanshan Normal University, Chaozhou, 521041, China
  2. Guangxi Botanical Garden of Medicinal Plants, Nanning, 530023, China
  3. The Second Affiliated Hospital, College of Medicine, Shantou University, Shantou, 515041, China
  
• ISSN：1976-3786

文摘

Ten lupeol dicarboxylic acid monoester derivatives as new potent antitumor agents were synthesized and evaluated for in vitro antitumor activities against A549, LAC, HepG2 and HeLa cell lines. Among them, compounds 1strong class="a-plus-plus">5 showed excellent antitumor activities against all tested tumor cell lines and compounds 6strong class="a-plus-plus">10 exhibited high activities against A549, HepG2 and HeLa cells, exceeded lupeol, lupanol and doxorubicin. Compound 2 displayed the highest potent antitumor activities with IC50 values of 5.78 against A549 cell, 2.38 against LAC cell, 6.14 against HepG2 cell and 0.00842 against HeLa cell.