Synthesis and antitumor activity of novel 3-oxo-23-hydroxybetulinic acid derivatives

Hengyuan Zhang, Peiqing Zhu, Jie Liu, Xue Yang, Shengtao Xu, Hequan Yao, Jieyun Jiang, Wencai Ye, Xiaoming Wu, Jinyi Xu

Research output: Contribution to journalArticlepeer-review

19 Scopus citations


A series of novel derivatives of 3-oxo-23-hydroxybetulinic acid was designed, synthesized, and evaluated for their antiproliferative activity against a panel of cancer cell lines (HL-60, BEL-7402, SF-763, HeLa, B16 and A375). The results indicated that majority of the derivatives exhibited more significant antitumor activity than the parent compound. In particular compound 10e showed the most potent activity with IC50values of 5.85, 6.23 and 7.22 μM against B16, SF-763 and BEL-7402 cells, respectively. Furthermore, 10e inhibited tumor growth by 51.8% and 62.7% (w/w) in H22 and B16 xenograft mouse models, comparable to cyclophosphamide and 5-fluorouracil, respectively.

Original languageEnglish
Pages (from-to)159-167
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
StatePublished - Nov 24 2014

Bibliographical note

Publisher Copyright:
© 2014 Elsevier Masson SAS.


  • 3-Oxo-23-hydroxybetulinic acid
  • Antiproliferative activity
  • Antitumor activity
  • B16 melanoma
  • Chemical modification

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


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