Fused thiophene derivatives as MEK inhibitors.

Victoria E Laing,Daniel C Brookings,Rachel J Carbery,Jose Gascon Simorte,Martin C Hutchings,Barry J Langham,Martin A Lowe,Rodger A Allen,Joanne R Fetterman,James Turner,Christoph Meier,Jeff Kennedy,Mark Merriman

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

A number of novel fused thiophene derivatives have been prepared and identified as potent inhibitors of MEK. The SAR data of selected examples and the in vivo profiling of compound 13h demonstrates the functional activity of this class of compounds in HT-29 PK/PD models.

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关键词

MEK,Non-ATP competitive MEK inhibitor,Allosteric MEK inhibitor

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