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

页码：8832 / 8841

页数：10