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学科主题: 药学
题名:
Substituted 3-Benzylcoumarins as Allosteric MEK1 Inhibitors: Design, Synthesis and Biological Evaluation as Antiviral Agents
作者: Wang, Chao1; Zhang, Hao2; Xu, Fengrong1; Niu, Yan1; Wu, Yun1; Wang, Xin2; Peng, Yihong2; Sun, Jing1; Liang, Lei1; Xu, Ping1
关键词: MEK1 inhibitor ; coumarin ; antiviral
刊名: MOLECULES
发表日期: 2013-05-01
DOI: 10.3390/molecules18056057
卷: 18, 期:5, 页:6057-6091
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Organic
研究领域[WOS]: Chemistry
关键词[WOS]: PROTEIN-KINASE KINASE ; SIMPLEX-VIRUS HSV-2 ; COUMARIN DERIVATIVES ; MEDICINAL CHEMISTRY ; REPLICATION ; PATHWAY ; FLUORINE ; IDENTIFICATION ; PROGRESS ; CASCADE
英文摘要:

In order to find novel antiviral agents, a series of allosteric MEK1 inhibitors were designed and synthesized. Based on docking results, multiple optimizations were made on the coumarin scaffold. Some of the derivatives showed excellent MEK1 binding affinity in the appropriate enzymatic assays and displayed obvious inhibitory effects on the ERK pathway in a cellular assay. These compounds also significantly inhibited virus (EV71) replication in HEK293 and RD cells. Several compounds showed potential as agents for the treatment of viral infective diseases, with the most potent compound 18 showing an IC50 value of 54.57 nM in the MEK1 binding assay.

语种: 英语
所属项目编号: 21172012 ; 2012CB518000 ; 2007AA02Z317 ; 20120001110010
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China ; National High-Tech Research and Development Program of China (863 Program) ; Specialized Research Fund for the Doctoral Program of Higher Education of China
WOS记录号: WOS:000319446900077
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/57915
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Hlth Sci Ctr, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs,Dept Med Chem, Beijing 100191, Peoples R China
2.Peking Univ, Dept Microbiol, Sch Basic Med Sci, Beijing 100191, Peoples R China

Recommended Citation:
Wang, Chao,Zhang, Hao,Xu, Fengrong,et al. Substituted 3-Benzylcoumarins as Allosteric MEK1 Inhibitors: Design, Synthesis and Biological Evaluation as Antiviral Agents[J]. MOLECULES,2013,18(5):6057-6091.
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