Synthesis and cytotoxicity of triterpenoids derived from betulin and betulinic acid via click chemistry

被引：24

作者：

Shi, Wei ^{[1
]}

Tang, Ning ^{[1
]}

Yan, Wei-Dong ^{[1
]}

机构：

[1] Zhejiang Univ, Dept Chem, Hangzhou 310027, Zhejiang, Peoples R China

来源：

JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH | 2015年 / 17卷 / 02期

基金：

中国国家自然科学基金;

关键词：

betulin; betulinic acid; cytotoxicity; derivatives; click chemistry; LUPANE TRITERPENOIDS; INHIBITOR; DERIVATIVES; PA-457; AGENTS;

D O I：

10.1080/10286020.2014.979164

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

In this study, a series of triazole substituted betulin and betulinic acid derivatives was designed and synthesized via click chemistry at C-30 position. Eighteen target compounds were evaluated in vitro for their antitumor activities against leukemia cell-line HL-60. Seventeen compounds have not reported before. The cytotoxic experiment showed that most of betulinic acid derived triazoles have higher cytotoxic profile than betulinic acid. Among them, compound 30-[4-(4-fluorophenyl)-1H-1,2,3-triazol-1-yl] betulinic acid (7b) showed the best IC50 value (1.3 mu M) against leukemia cell-line HL-60 (eight- to ninefold higher potency than betulinic acid).

引用

页码：159 / 169

页数：11

共 23 条

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