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

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Abstract

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 1–5 showed excellent antitumor activities against all tested tumor cell lines and compounds 6–10 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 μM against A549 cell, 2.38 μM against LAC cell, 6.14 μM against HepG2 cell and 0.00842 μM against HeLa cell.

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Acknowledgments

The study was supported by grants from the Natural Science Foundation of Hanshan Normal University (No. QD20110616) and the Basic and Clinical Research Foundation of Medical College of Shantou University (No. LD030601).

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Authors and Affiliations

  1. Department of Chemistry, Hanshan Normal University, Chaozhou, 521041, China

    Weijie Li

  2. Guangxi Botanical Garden of Medicinal Plants, Nanning, 530023, China

    Jing Hao

  3. The Second Affiliated Hospital, College of Medicine, Shantou University, Shantou, 515041, China

    Yeyu Xiao

Authors
  1. Weijie Li
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  2. Jing Hao
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  3. Yeyu Xiao
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Corresponding author

Correspondence to Weijie Li.

Additional information

Weijie Li and Yeyu Xiao were contributed equally to this study.

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Li, W., Hao, J. & Xiao, Y. Synthesis and in vitro antitumor activities of lupeol dicarboxylic acid monoester derivatives. Arch. Pharm. Res. 36, 1447–1453 (2013). https://doi.org/10.1007/s12272-013-0155-x

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  • DOI: https://doi.org/10.1007/s12272-013-0155-x

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