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2-Amino-aryl-7-aryl-benzoxazoles as Potent, Selective and Orally Available JAK2 Inhibitors

Gerspacher, Marc and Furet, Pascal and Pissot Soldermann, Carole and Gaul, Christoph and Holzer, Philipp and Vangrevelinghe, Eric and Lang, Marc and Buhl, Thomas and Aichholz, Reiner and Blasco, Francesca and Endres, Ralf and Erdmann, Dirk and Radimerski, Thomas and Regnier, Catherine and Chene, Patrick and Hofmann, Francesco and Trappe, Joerg and Drueckes, Peter and Baffert, Fabienne and De Pover, Alain (2010) 2-Amino-aryl-7-aryl-benzoxazoles as Potent, Selective and Orally Available JAK2 Inhibitors. Bioorganic & Medicinal Chemistry Letters, 20 (5). pp. 1724-1727. ISSN 0960-894X


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.

Item Type: Article
Related URLs:
Additional Information: Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Janus kinase; JAK1; JAK2; JAK3; Tyk2; Kinase inhibitors; JAK2 inhibitor
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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16


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