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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
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 / Revised: 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 (CC BY 3.0).
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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.

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