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Novel Syk inhibitors with high potency in presence of blood

Thoma, Gebhard and Blanz, Joachim and Drueckes, Peter and Kittelmann, Matthias and Smith, Alexander Baxter and Van Eis, Maurice and Vangrevelinghe, Eric and Zerwes, Hans-Guenter and Che, Jianwei and He, Xiaohui and Jin, Yunho and Lee, Christian and Michellys, Pierre and Uno, Tetsuo and Liu, Hong and Buehlmayer, Peter (2014) Novel Syk inhibitors with high potency in presence of blood. Bioorganic and Medicinal Chemistry Letters, 24. pp. 2278-2282.


We describe two series of Syk inhibitors which potently abrogate Syk kinase function in enzymatic, 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).

Item Type: Article
Date Deposited: 13 Oct 2015 13:13
Last Modified: 13 Oct 2015 13:13


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