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Synthesis, antitumor activity and mechanism of action of novel 1,3-thiazole derivatives containing hydrazide-hydrazone and carboxamide moiety

文献类型： 外文期刊

作者： He, Haifeng 1 ; Wang, Xiaoyan 1 ; Shi, Liqiao 2 ; Yin, Wenyan 2 ; Yang, Ziwen 2 ; He, Hongwu 1 ; Liang, Ying 2 ;

作者机构： 1.Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China

2.Hubei Acad Agr Sci, Natl Biopesticide Engn Res Ctr, Wuhan 430064, Peoples R China

关键词： 1,3-Thiazole;Carboxamide;Hydrazide-hydrazone;Antitumor activity;Apoptosis

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

ISSN： 0960-894X

年卷期： 2016 年 26 卷 14 期

页码：

收录情况： SCI

摘要： A series of novel 2,4,5-trisubstituted 1,3-thiazole derivatives containing hydrazide-hydrazine, and carboxamide moiety including 46 compounds T were synthesized, and evaluated for their antitumor activity in vitro against a panel of five human cancer cell lines. Eighteen title compounds T displayed higher inhibitory activity than that of 5-Fu against MCF-7, HepG2, BGC-823, Hela, and A549 cell lines. Especially, T1, T26 and T38 exhibit best cytotoxic activity with IC50 values of 2.21 mu g/mL, 1.67 mu g/mL and 1.11 mu g/mL, against MCF-7, BCG-823, and HepG2 cell lines, respectively. These results suggested that the combination of 1,3-thiazole, hydrazide-hydrazone, and carboxamide moiety was much favorable to cytotoxicity activity. Furthermore, the flow cytometry analysis revealed that compounds T1 and T38 could induce apoptosis in HepG2 cells, and it was confirmed T38 led the induction of cell apoptosis by S cell-cycle arrest. (C) 2016 Elsevier Ltd. All rights reserved.

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