Design, Synthesis, Biological Activity and Molecular Docking Study of Coumarin Derivatives Bearing 2-Methylbiphenyl Moiety
文献类型：期刊论文
| 作者 | Ma Junjie2; Huang Kun2; Ni Xin2; Chen Roufen2; Xu Boxuan3; Wang Cuifang1 |
| 刊名 | CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
 |
| 出版日期 | 2019 |
| 卷号 | 35期号:3页码:410-417 |
| 关键词 | GROWTH POTENT Coumarin 2-Methylbiphenyl Anticancer activity PD-1/PD-L1 inhibitory activity Molecular docking |
| ISSN号 | 1005-9040 |
| 其他题名 | Design, Synthesis, Biological Activity and Molecular Docking Study of Coumarin Derivatives Bearing 2-Methylbiphenyl Moiety |
| 英文摘要 | A hybrid pharmacophore approach was used to design and synthesize a series of coumarin derivatives bearing 2-methylbiphenyl moiety, which were evaluated for their in vitro anticancer activities against four cancer cell lines(MCF-7, A549, H460 and HT29) and PD-1/PD-L1 inhibitory activities. Moreover, several compounds with excellent anticancer activities were selected to evaluate the cytotoxicities against one normal cell line(HEK-293). The most promising compound 11o showed the best anticancer activities against the four tested cancer cell lines with the IC50 values of 6.45, 8.65, 6,57 and 8.13 mu mol/L, respectively, and displayed weak cytotoxicity on the normal cell(HEK-293). Furthermore, screening of PD-1/PD-L1 inhibitory activity revealed that compound 11o could effectively inhibit the binding of PD-1/PD-L1, and the binding interactions of compound 11o with PD-L1 protein were explored by molecular docking. All above evidences showed that compound 11o might be worthy of further study as a valuable leading compound for the treatment of cancer. |
| 资助项目 | [National Natural Science Foundation of China] ; [Promotion Program for Young and Middle-aged Teacher in Science and Technology Research of Huaqiao University, China] ; [Science and Technology Project of Quanzhou City, China] ; [Subsidized Project for Postgraduates' Innovative Fund in Scientific Research of Huaqiao University, China] |
| 语种 | 英语 |
| CSCD记录号 | CSCD:6505899 |
| 源URL | [http://ir.imr.ac.cn/handle/321006/89644]  |
| 专题 | 金属研究所_中国科学院金属研究所 |
| 作者单位 | 1.泉州师范学院 2.华侨大学 3.中国科学院金属研究所 |
| 推荐引用方式 GB/T 7714 | Ma Junjie,Huang Kun,Ni Xin,et al. Design, Synthesis, Biological Activity and Molecular Docking Study of Coumarin Derivatives Bearing 2-Methylbiphenyl Moiety[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2019,35(3):410-417. |
| APA | Ma Junjie,Huang Kun,Ni Xin,Chen Roufen,Xu Boxuan,&Wang Cuifang.(2019).Design, Synthesis, Biological Activity and Molecular Docking Study of Coumarin Derivatives Bearing 2-Methylbiphenyl Moiety.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,35(3),410-417. |
| MLA | Ma Junjie,et al."Design, Synthesis, Biological Activity and Molecular Docking Study of Coumarin Derivatives Bearing 2-Methylbiphenyl Moiety".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 35.3(2019):410-417. |
入库方式： OAI收割
来源：金属研究所
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