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

Yi Bi 1 , Jinyi Xu 2,3,* email, Fei Sun 2 , Xiaoming Wu 3,* email, Wencai Ye 4 , Yijun Sun 5  and Wenwen Huang 1
1 School of Pharmacy, Yantai University, Yantai 264005, Shandong, China 2 Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, Jiangsu, China 3 State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, Jiangsu, China 4 Department of Phytochemistry, China Pharmaceutical University, Nanjing 210009, Jiangsu, China 5 Drug Screening Center, Nanjing KeyGen Biotech. Co. Ltd., Nanjing 210012, Jiangsu, China
* Authors to whom correspondence should be addressed.
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

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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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