Synthesis and Biological Evaluation of Novel Betulin Derivatives with Aromatic Hydrazone Side Chain as Potential Anticancer Agents

被引:8
作者
Wang, Jiafeng [1 ]
Wu, Jiale [1 ]
Han, Yinglong [1 ]
Zhang, Jie [1 ]
Lin, Yu [1 ]
Wang, Haijun [1 ]
Wang, Jing [1 ]
Bu, Ming [1 ]
机构
[1] Qiqihar Med Univ, Coll Pharm, Qiqihar 161006, Peoples R China
关键词
betulin derivatives; hydrazone; heterocycles; antitumor; apoptosis; IN-VITRO; HETEROCYCLES; ACID;
D O I
10.21577/0103-5053.20210140
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of novel betulin-28-hydrazone derivatives (7a-7o) were synthesized. All compounds were evaluated for their in vitro cytotoxicities in four human carcinoma cells (HepG2, MCF-7, HCT-116 and A549). Among them, compound 7l displayed the most potent cytotoxicity with an IC50 (concentration of the tested compound that inhibits 50% of cell growth) value of 7.37 +/- 0.38 mu M against MCF-7 cells. The preliminary cellular mechanism studies indicated that compound 7l could induce MCF-7 cells apoptosis. The above findings indicated that compound 7l may be used as a lead compound for antitumor agents with improved efficacy.
引用
收藏
页码:227 / +
页数:41
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