Synthesis and Cytotoxic Activity of Novel Betulin Derivatives Containing Hydrazide-Hydrazone Moieties

被引：5

作者：

Wu, Jiale ^{[1
]}

Wang, Jiafeng ^{[1
]}

Han, Yinglong ^{[1
]}

Lin, Yu ^{[1
]}

Wang, Jing ^{[1
]}

Bu, Ming ^{[1
]}

机构：

[1] Qiqihar Med Univ, Coll Pharm, Qiqihar 161006, Peoples R China

来源：

NATURAL PRODUCT COMMUNICATIONS | 2021年 / 16卷 / 10期

关键词：

betulin; hydrazide; hydrazone; derivatives; antitumor activity; ANALOGS; ACID; TETRAHYDROCURCUMIN; AGENTS;

D O I：

10.1177/1934578X211055345

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel betulin derivatives containing hydrazide-hydrazone moieties were synthesized. All compounds were evaluated for their cytotoxicity against four human carcinoma cell lines (HepG2, A549, MCF-7 and HCT-116) and a normal human gastric epithelial cell line (GES-1). Among them, compound 6i was the most potent against HepG2 and MCF-7 cell lines, with IC50 values of 9.27 and 8.87 mu M, respectively. The results suggest that the incorporation of a hydrazide-hydrazone side chain at the C-28 position of betulin is beneficial for compounds to display significant cytotoxicity. Compound 6i may be used as a promising skeleton for antitumor agents with improved efficacy.

引用

页数：7

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