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Novel Syk inhibitors with high potency in presence of blood

Thoma, Gebhard, Blanz, Joachim, Drueckes, Peter, Kittelmann, Matthias, Smith, Alexander Baxter, Van Eis, Maurice, Vangrevelinghe, Eric, Zerwes, Hans-Guenter, Che, Jianwei, He, Xiaohui, Jin, Yunho, Lee, Christian, Michellys, Pierre, Uno, Tetsuo, 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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