Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents
Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents
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作为潜在抗癌剂的新型 1,2,3-三唑-二硫代氨基甲酸酯杂化物的设计和合成
DOI：
10.1016/j.ejmech.2012.12.046
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发表时间：
2013-04-01
影响因子：
6.7
通讯作者：
Liu, Hong-Min
中科院分区：
文献类型：
--
作者：
Duan, Ying-Chao;Ma, Yong-Cheng;Liu, Hong-Min
设计、合成了一系列新型的1，2，3-三唑-二硫代氨基甲酸酯杂环化合物，并对4种人肿瘤细胞株（MGC-803、MCF-7、PC-3、EC-109）进行了体外抗肿瘤活性评价。大多数合成的化合物对MGC-803和MCF-7表现出中等至有效的活性。其中，化合物3a和3c显示出优异的广谱抗癌活性，其IC 50值分别为0.73 - 11.61 μ M和0.49-12.45 μ M。特别地，化合物3a比5-氟尿嘧啶对所有测试的人癌细胞系更有效。流式细胞仪分析表明，3c处理MGC-803导致细胞周期停滞在G2/M期，并在12 h后增加凋亡细胞死亡。(C)2013年Elsevier Masson SAS。All rights reserved.
A series of novel 1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for anticancer activity against four selected human tumor cell lines (MGC-803, MCF-7, PC-3, EC-109). Majority of the synthesized compounds exhibited moderate to potent activity against MGC-803 and MCF-7. Among them, compounds 3a and 3c showed excellent broad spectrum anticancer activity with IC50 values ranging from 0.73 to 11.61 mu M and 0.49-12.45 mu M, respectively. Particularly, compound 3a was more potent than 5-fluorouracil against all tested human cancer cell lines. Flow cytometry analysis demonstrated that treatment of MGC-803 with 3c led to cell cycle arrest at G2/M phase accompanied by an increase in apoptotic cell death after 12 h. (C) 2013 Elsevier Masson SAS. All rights reserved.