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

被引：18
作者：
Bi, Yi [2 ]
Xu, Jinyi [1 ,3 ]
Sun, Fei [1 ]
Wu, Xiaoming [3 ]
Ye, Wencai [4 ]
Sun, Yijun [5 ]
Huang, Wenwen [2 ]
机构：
[1] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China
[2] Yantai Univ, Sch Pharm, Yantai 264005, Shandong, Peoples R China
[3] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
[4] China Pharmaceut Univ, Dept Phytochem, Nanjing 210009, Jiangsu, Peoples R China
[5] Nanjing KeyGen Biotech Co Ltd, Drug Screening Ctr, Nanjing 210012, Jiangsu, Peoples R China
来源：
MOLECULES | 2012年 / 17卷 / 08期
关键词：
23-hydroxybetulinic acid; C-28 ester derivatives; antitumor activity; structure-activity relationships; BETULINIC ACID;
D O I：
10.3390/molecules17088832
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 mu M in HL-60 cells and showed similar antitumor activity as cyclophosphamide in H22 liver tumor and as 5-fluorouracil in B16 melanoma in vivo.
引用
收藏
页码：8832 / 8841
页数：10
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