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Substituted 3-benzylcoumarins as allosteric MEK1 inhibitors: design, synthesis and biological evaluation as antiviral agents.

ABSTRACT: 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 IC?? value of 54.57 nM in the MEK1 binding assay.

SUBMITTER: Wang C 

PROVIDER: S-EPMC6269873 | biostudies-literature | 2013 May

REPOSITORIES: biostudies-literature

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Substituted 3-benzylcoumarins as allosteric MEK1 inhibitors: design, synthesis and biological evaluation as antiviral agents.

Wang Chao C   Zhang Hao H   Xu Fengrong F   Niu Yan Y   Wu Yun Y   Wang Xin X   Peng Yihong Y   Sun Jing J   Liang Lei L   Xu Ping P  

Molecules (Basel, Switzerland) 20130521 5

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 poten  ...[more]

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