Design, synthesis and anticancer activity of novel nopinone-based thiosemicarbazone derivatives
Design, synthesis and anticancer activity of novel nopinone-based thiosemicarbazone derivatives
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新型诺吡酮基缩氨基硫脲衍生物的设计、合成及其抗癌活性
DOI：
10.1016/j.bmcl.2017.04.024
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发表时间：
2017-06-01
影响因子：
2.7
通讯作者：
Wang, Shifa
中科院分区：
文献类型：
--
作者：
Wang, Yunyun;Gu, Wen;Wang, Shifa
设计并合成了一系列基于诺品酮的缩氨基硫脲类化合物。所有化合物均经H-1 NMR、C-13 NMR、HR-MS谱分析鉴定。在体外抗癌活性中，大多数衍生物对三种人癌细胞系（MDA-MB-231，SMMC-7721和Hela）显示出相当大的细胞毒活性。其中化合物4 i对三种癌细胞系显示出最强的抗肿瘤活性，其IC 50值分别为2.79 ± 0.38、2.64 ± 0.17和3.64 ± 0.13 μ M。细胞周期分析表明，化合物4 i使MDA-MB-231细胞周期阻滞于G2/M期。Annexin V-FITC/7-AAD双染法也显示化合物4 i诱导MDA-MB-231细胞早期凋亡。(C)2017爱思唯尔有限公司版权所有
A series of new nopinone-based thiosemicarbazone derivatives were designed and synthesized as potent anticancer agents. All these compounds were identified by H-1 NMR, C-13 NMR, HR-MS spectra analyses. In the in vitro anticancer activity, most derivatives showed considerable cytotoxic activity against three human cancer cell lines (MDA-MB-231, SMMC-7721 and Hela). Among them, compound 4i exhibited most potent antitumor activity against three cancer cell lines with the IC50 values of 2.79 +/- 0.38, 2.64 +/- 0.17 and 3.64 +/- 0.13 mu M, respectively. Furthermore, the cell cycle analysis indicated that compound 4i caused cell cycle arrest of MDA-MB-231 cells at G2/M phase. The Annexin V-FITC/7-AAD dual staining assay also revealed that compound 4i induced the early apoptosis of MDA-MB-231 cells. (C) 2017 Elsevier Ltd. All rights reserved.