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

Gerspacher, Marc, Furet, Pascal, Pissot Soldermann, Carole, Gaul, Christoph, Holzer, Philipp, Vangrevelinghe, Eric, Lang, Marc, Buhl, Thomas, Aichholz, Reiner, Blasco, Francesca, Endres, Ralf, Erdmann, Dirk, Radimerski, Thomas, Regnier, Catherine, Chene, Patrick, Hofmann, Francesco, Trappe, Joerg, Drueckes, Peter, 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
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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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