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Substituted 3-Benzylcoumarins as Allosteric MEK1 Inhibitors: Design, Synthesis and Biological Evaluation as Antiviral Agents
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
2013-05-01
DOI10.3390/molecules18056057
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
WOS记录号WOS:000319446900077
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/57915
专题北京大学药学院
北京大学基础医学院
北京大学药学院_药物化学系
北京大学第二临床医学院_消化科
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
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GB/T 7714
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.
APA Wang, Chao.,Zhang, Hao.,Xu, Fengrong.,Niu, Yan.,Wu, Yun.,...&Xu, Ping.(2013).Substituted 3-Benzylcoumarins as Allosteric MEK1 Inhibitors: Design, Synthesis and Biological Evaluation as Antiviral Agents.MOLECULES,18(5),6057-6091.
MLA Wang, Chao,et al."Substituted 3-Benzylcoumarins as Allosteric MEK1 Inhibitors: Design, Synthesis and Biological Evaluation as Antiviral Agents".MOLECULES 18.5(2013):6057-6091.
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