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Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors

Pissot Soldermann, Carole and Gerspacher, Marc and Gaul, Christoph and Holzer, Philipp and Radimerski, Thomas and Regnier, Catherine and Baffert, Fabienne and Drueckes, Peter and Tavares, Gisele and Furet, Pascal and Vangrevelinghe, Eric and Blasco, Francesca and Ottaviani, Giorgio and Ossola, Flavio and Scesa, Julien and Reetz, Janitha (2010) Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors. Bioorganic and Medicinal Chemistry Letters, 20 (8). pp. 2609-2613. ISSN 0960-894X

Abstract

We have designed and synthesized a novel series of 2,8-diaryl-quinoxalines as Janus kinase 2 inhibitors. Many of the inhibitors show low nanomolar activity against JAK2 and potently suppress proliferation of SET-2 cells in vitro. In addition, the compounds have favorable rat pharmacokinetic properties suitable for in vivo efficacy evaluation.

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
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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16
URI: https://oak.novartis.com/id/eprint/1918

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