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An orally bioavailable Syk inhibitor with activity in a rat PK/PD model

Thoma, Gebhard and Veenstra, Siem and Strang, Ross and Blanz, Joachim and Vangrevelinghe, Eric and Berghausen, Joerg and Lee, Christian and Zerwes, Hans-Guenter (2015) An orally bioavailable Syk inhibitor with activity in a rat PK/PD model. Bioorganic and Medicinal Chemistry Letters.

Abstract

Design and optimization of benzo and pyridothiazoles and 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. But 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.

Item Type: Article
Date Deposited: 13 Oct 2015 13:11
Last Modified: 13 Oct 2015 13:11
URI: https://oak.novartis.com/id/eprint/26656

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