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

C Pissot-Soldermann, M Gerspacher, P Furet…

文献索引：Pissot-Soldermann, Carole; Gerspacher, Marc; Furet, Pascal; Gaul, Christoph; Holzer, Philipp; McCarthy, Clive; Radimerski, Thomas; Regnier, Catherine H.; Baffert, Fabienne; Drueckes, Peter; Tavares, Gisele A.; Vangrevelinghe, Eric; Blasco, Francesca; Ottaviani, Giorgio; Ossola, Flavio; Scesa, Julien; Reetz, Janitha Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 8 p. 2609 - 2613

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被引用次数: 26

摘要

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, compounds from this series have favorable rat pharmacokinetic properties suitable for in vivo efficacy evaluation.