Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Basic Information
ID: ALA3621151
Journal: Bioorg Med Chem Lett
Title: Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Authors: Thoma G, Veenstra S, Strang R, Blanz J, Vangrevelinghe E, Berghausen J, Lee CC, Zerwes HG.
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.
CiteXplore: 26320624
DOI: 10.1016/j.bmcl.2015.08.037
Patent ID: ┄