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

@article{Wang2013Substituted3A,
  title={Substituted 3-benzylcoumarins as allosteric MEK1 inhibitors: design, synthesis and biological evaluation as antiviral agents.},
  author={Chao Wang and Hao Zhang and Fengrong Xu and Yan Niu and Yun Wu and Xin Wang and Yihong Peng and Jing Sun and Lei Liang and Ping Xu},
  journal={Molecules},
  year={2013},
  volume={18 5},
  pages={6057-91}
}
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… CONTINUE READING

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