Design, synthesis and antiproliferative activity studies of novel dithiocarbamate-chalcone derivates
Design, synthesis and antiproliferative activity studies of novel dithiocarbamate-chalcone derivates
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新型二硫代氨基甲酸酯-查耳酮衍生物的设计、合成和抗增殖活性研究
DOI：
10.1016/j.bmcl.2016.07.012
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发表时间：
2016-08-15
影响因子：
2.7
通讯作者：
Zhang, Yan-Bing
中科院分区：
文献类型：
--
作者：
Fu, Dong-Jun;Zhang, Sai-Yang;Zhang, Yan-Bing
设计、合成了一系列新的二硫代氨基甲酸酯-查耳酮衍生物，并对三种选定的癌细胞系（EC-109、SK-N-SH和MGC-803）进行了抗增殖活性评价。大多数合成的化合物对所有测定的癌细胞系表现出中等至有效的活性。特别地，化合物II 2和II 5对SK-N-SH表现出优异的生长抑制作用，其IC 50值分别为2.03 μ M和2.46 μ M。进一步的机制研究表明，化合物II 2可通过诱导细胞凋亡，使细胞周期阻滞于G 0/G1期，从而明显抑制SK-N-SH细胞的增殖。(C)2016爱思唯尔有限公司版权所有
A series of novel dithiocarbamate-chalcone derivates were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell lines (EC-109, SK-N-SH and MGC-803). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds II2 and II5 exhibited the excellent growth inhibition against SK-N-SH with IC50 values of 2.03 mu M and 2.46 mu M, respectively. Further mechanism studies revealed that compound II2 could obviously inhibit the proliferation of SK-N-SH cells by inducing apoptosis and arresting the cell cycle at G0/G1 phase. (C) 2016 Elsevier Ltd. All rights reserved.