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Molecules 2012, 17(8), 8832-8841; doi:10.3390/molecules17088832
Article

Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates

1, 2,3,* , 2, 3,* , 4, 5 and 1
Received: 29 May 2012; in revised form: 17 July 2012 / Accepted: 18 July 2012 / Published: 25 July 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract: 23-Hydroxybetulinic acid (1) served as the precursor for the synthesis of C-28 ester derivatives. The target compounds were evaluated in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60). Among the obtained compounds, 6i had the most potent antitumor activity, with the IC50 values of 8.35 µM in HL-60 cells and showed similar antitumor activity as cyclophosphamide in H22 liver tumor and as 5-fluorouracil in B16 melanoma in vivo.
Keywords: 23-hydroxybetulinic acid; C-28 ester derivatives; antitumor activity; structure-activity relationships 23-hydroxybetulinic acid; C-28 ester derivatives; antitumor activity; structure-activity relationships
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Bi, Y.; Xu, J.; Sun, F.; Wu, X.; Ye, W.; Sun, Y.; Huang, W. Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates. Molecules 2012, 17, 8832-8841.

AMA Style

Bi Y, Xu J, Sun F, Wu X, Ye W, Sun Y, Huang W. Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates. Molecules. 2012; 17(8):8832-8841.

Chicago/Turabian Style

Bi, Yi; Xu, Jinyi; Sun, Fei; Wu, Xiaoming; Ye, Wencai; Sun, Yijun; Huang, Wenwen. 2012. "Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates." Molecules 17, no. 8: 8832-8841.



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