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

23-Hydroxybetulinic acid (<strong>1</strong>) served as the precursor for the synthesis of C-28 ester derivatives. The target compounds were evaluated <em>in vitro</em> for their antitumor activities against five cell lines (A549, BEL-7402, SF-...

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Bibliographic Details
Main Authors: Yijun Sun, Wencai Ye, Xiaoming Wu, Fei Sun, Jinyi Xu, Yi Bi, Wenwen Huang
Format: Article
Language:English
Published: MDPI AG 2012-07-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/17/8/8832
Description
Summary:23-Hydroxybetulinic acid (<strong>1</strong>) served as the precursor for the synthesis of C-28 ester derivatives. The target compounds were evaluated <em>in vitro</em> for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60)<em>.</em> Among the obtained compounds, <strong>6i</strong> had the most potent antitumor activity, with the IC<sub>50</sub> 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<em> in vivo</em>.
ISSN:1420-3049