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ID: ALA3259804

Journal: Bioorg Med Chem Lett

Title: Syk inhibitors with high potency in presence of blood.

Authors: Thoma G, Blanz J, Bühlmayer P, Drückes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H.

Abstract: 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).

CiteXplore: 24726806

DOI: 10.1016/j.bmcl.2014.03.075