Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action

文献类型： 外文期刊

第一作者： Yu, Xifang

作者： Yu, Xifang;Shi, Liqiao;Ke, Shaoyong

作者机构：

关键词： Acylhydrazone;Synthesis;Cytotoxic activity;Apoptosis

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS （ 影响因子：2.823； 五年影响因子：2.677 ）

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收录情况： SCI

摘要： A series of novel acylhydrazone derivatives were designed, synthesized and evaluated for their potential cytotoxic effects against human cancer cell lines. The preliminary results indicated that some of the obtained compounds (such as 8b, 13c) exhibited good to moderate cytotoxic activities against human HepG2, Huh-7, and BCG-823 cell lines. Especially, compounds 8c and 8e presented obviously selective cytotoxic activities against Huh-7 in vitro (8c, IC50 = 7.74 +/- 2.18 mu g/mL; 8e, IC50 = 4.46 +/- 1.05 mu g/mL) compared to 5-FU (IC50 = 10.41 +/- 3.41 mu g/mL). The highly potential compounds to induce apoptosis in HepG2 cells were analyzed by flow cytometry, and the apoptotic effects of compounds 8b and 13c were further evaluated using Annexin V-FITC/propidium iodide dual staining assay. (C) 2015 Elsevier Ltd. All rights reserved.

分类号： R9

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