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2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

Authors :
Christoph Gaul
Patrick Chène
Thomas Radimerski
Eric Vangrevelinghe
Carole Pissot-Soldermann
Alain De Pover
Marc Gerspacher
Ralf Endres
Dirk Erdmann
Fabienne Baffert
Francesco Hofmann
Jörg Trappe
Peter Drueckes
Marc Lang
Thomas Buhl
Reiner Aichholz
Catherine H. Régnier
Francesca Blasco
Philipp Holzer
Pascal Furet
Source :
Bioorganicmedicinal chemistry letters. 20(5)
Publication Year :
2009

Abstract

A series of novel benzoxazole derivatives has been designed and shown to exhibit attractive JAK2 inhibitory profiles in biochemical and cellular assays, capable of delivering compounds with favorable PK properties in rats. Synthesis and structure–activity relationship data are also provided.

Details

ISSN :
14643405
Volume :
20
Issue :
5
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry letters
Accession number :
edsair.doi.dedup.....8bddf41be25aecaef0f06f28d246bf79