The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.

Kai Schiemann,Dirk Finsinger,Frank Zenke,Christiane Amendt,Thorsten Knöchel,David Bruge,Hans-Peter Buchstaller,Ulrich Emde,Wolfgang Stähle,Soheila Anzali

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

The synthesis, SAR, co-crystal structure and in vivo activity of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5 are described.

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关键词

Kinesin-5,Eg5 inhibitors,Kinesin spindle protein,KSP,Anti mitotic agents,SAR,EMD 534085

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