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Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.

Thoma G, Veenstra S, Strang R, Blanz J, Vangrevelinghe E, Berghausen J, Lee CC, Zerwes HG
Bioorg Med Chem Lett 25 4642-7 (2015)
Related entries: 5cxz, 5cy3

Cited: 4 times
EuropePMC logo PMID: 26320624

Abstract

Design and optimization of benzo- and pyrido-thiazoles/isothiazoles are reported leading to the discovery of the potent, orally bioavailable Syk inhibitor 5, which was found to be active in a rat PK/PD model. Compound 5 showed acceptable overall kinase selectivity. However, in addition to Syk it also inhibited Aurora kinase in enzymatic and cellular settings leading to findings in the micronucleus assay. As a consequence, compound 5 was not further pursued.

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