Syk inhibitors with high potency in presence of blood.

Bioorganic & medicinal chemistry letters ·Vol. 24 ·No. 10 ·2015-02-20

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

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).

Keywords

Aldehyde oxidase BIIB-057 Fostamatinib Kinase inhibitors Spleen tyrosine kinase

Article Info

Journal

Bioorganic & medicinal chemistry letters

Abbr.

Bioorg Med Chem Lett

ISSN

0960-894X

DOI

10.1016/j.bmcl.2014.03.075

Published

2015-02-20

Indexed

2014-04-30

Updated

2016-11-25

Language

English

Country/Region

England

NLM ID

9107377

External Links

PubMed source DOI: 10.1016/j.bmcl.2014.03.075 View journal details

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