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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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
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author Yijun Sun
Wencai Ye
Xiaoming Wu
Fei Sun
Jinyi Xu
Yi Bi
Wenwen Huang
author_facet Yijun Sun
Wencai Ye
Xiaoming Wu
Fei Sun
Jinyi Xu
Yi Bi
Wenwen Huang
author_sort Yijun Sun
collection DOAJ
description 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>.
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spelling doaj.art-52407bc43e3d4d548fa5a8e55ff98aac2022-12-22T02:44:58ZengMDPI AGMolecules1420-30492012-07-011788832884110.3390/molecules17088832Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent CandidatesYijun SunWencai YeXiaoming WuFei SunJinyi XuYi BiWenwen Huang23-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>.http://www.mdpi.com/1420-3049/17/8/883223-hydroxybetulinic acidC-28 ester derivativesantitumor activitystructure-activity relationships
spellingShingle Yijun Sun
Wencai Ye
Xiaoming Wu
Fei Sun
Jinyi Xu
Yi Bi
Wenwen Huang
Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates
Molecules
23-hydroxybetulinic acid
C-28 ester derivatives
antitumor activity
structure-activity relationships
title Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates
title_full Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates
title_fullStr Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates
title_full_unstemmed Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates
title_short Synthesis and Biological Activity of 23-Hydroxybetulinic Acid C-28 Ester Derivatives as Antitumor Agent Candidates
title_sort synthesis and biological activity of 23 hydroxybetulinic acid c 28 ester derivatives as antitumor agent candidates
topic 23-hydroxybetulinic acid
C-28 ester derivatives
antitumor activity
structure-activity relationships
url http://www.mdpi.com/1420-3049/17/8/8832
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