[1]黄险峰,沈梦兰,张诚,等.7-硫代黄酮衍生物的合成及其抗癌活性评价[J].常州大学学报(自然科学版),2016,(06):7-13.[doi:10.3969/j.issn.2095-0411.2016.06.002]
　HUANG Xianfeng,SHEN Menglan,ZHANG Cheng,et al.Synthesis and Biological Evaluation of Novel 7-Thioflavones as Anticancer Agents[J].Journal of Changzhou University(Natural Science Edition),2016,(06):7-13.[doi:10.3969/j.issn.2095-0411.2016.06.002]
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7-硫代黄酮衍生物的合成及其抗癌活性评价()
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常州大学学报(自然科学版)[ISSN:2095-0411/CN:32-1822/N]

卷:
期数:
2016年06期
页码:
7-13
栏目:
生物医学工程
出版日期:
2016-11-30

文章信息/Info

Title:
Synthesis and Biological Evaluation of Novel 7-Thioflavones as Anticancer Agents
作者:
黄险峰1; 沈梦兰1; 张诚2; 宋国强1
1. 常州大学 制药与生命科学学院,江苏 常州 213164; 2. 中山大学 药学院,广东 广州 510275
Author(s):
HUANG Xianfeng1;  SHEN Menglan1;  ZHANG Cheng2;  SONG Guoqiang1
1. School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China; 2. School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510275, China
关键词:
7-硫代黄酮;  粘着斑酶;  抗肿瘤活性
Keywords:
7-thioflavone;  FAK;  antitumor activity
分类号:
TK 8
DOI:
10.3969/j.issn.2095-0411.2016.06.002
文献标志码:
A
摘要:
合成了一系列新的7-硫代黄酮类化合物(5a～5l),通过MS、NMR等手段确定了化合物的结构,并且测试它们对粘着斑酶的抑制活性和对两种肿瘤细胞株的毒性。结果表明,化合物5l表现出较好的抗肿瘤活性,对人黑色素瘤细胞系和人肝癌细胞系的半数抑制浓度(IC50)分别为1.02 μmol/L和1.27 μmol/L。此外,5l也表现出很强的FAK抑制活性(IC50达到0.82 μmol/L)。还采用DS 2.5软件模拟对接,初步研究了5l和FAK(PDB code:2ETM)的结合模式。
Abstract:
A series of novel 7-thioflavones(5a-5l)have been designed and synthesized, their biological activities were also evaluated as potential antitumor and focal adhesion kinase FAK inhibitors. The bioassay assays demonstrated that compounds 5l showed potent activity,which inhibited the growth of B16-F10 and HepG2 cell lines with IC50 values of 1.02 μmol/L and 1.27 μmol/L. In addition, compound 5l also exhibited inhibitory activity against FAK(c(IC50)=0.82 μmol/L). Docking simulation was performed to insert compound 5l into the active site of FAK to determine the probable binding model. Based on the preliminary results, compound 5l with potent inhibitory activity in tumor growth may be a potential anticancer agent.

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备注/Memo

备注/Memo:
收稿日期:2016-06-04。基金项目:江苏省青年自然科学基金资助项目(BK20130248)。作者简介:黄险峰(1980—),男,湖北孝感人,博士,副教授,主要从事药物化学研究。
更新日期/Last Update: 2016-11-20