Syk inhibitors with high potency in presence of blood.

Gebhard Thoma,Joachim Blanz,Peter Bühlmayer,Peter Drückes,Matthias Kittelmann,Alexander B Smith,Maurice van Eis,Eric Vangrevelinghe,Hans-Günter Zerwes,Jianwei John Che,Xiaohui He,Yunho Jin,Christian C Lee,Pierre-Yves Michellys,Tetsuo Uno,Hong Liu

Bioorganic & Medicinal Chemistry Letters（2014）

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摘要

We describe two series of Syk inhibitors which potently abrogate Syk kinase function in enzymatic assays, cellular assays and in primary cells in the presence of blood. Introduction of a 7-aminoindole substituent led to derivatives with good kinase selectivity and little or no hERG channel inhibition (3b, 10c). (C) 2014 Elsevier Ltd. All rights reserved.

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关键词

Spleen tyrosine kinase,Aldehyde oxidase,Fostamatinib,BIIB-057,Kinase inhibitors

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