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

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

Bioorganic & medicinal chemistry letters (2010-03-17)
Carole Pissot-Soldermann, Marc Gerspacher, Pascal Furet, Christoph Gaul, Philipp Holzer, Clive McCarthy, Thomas Radimerski, Catherine H Regnier, Fabienne Baffert, Peter Drueckes, Gisele A Tavares, Eric Vangrevelinghe, Francesca Blasco, Giorgio Ottaviani, Flavio Ossola, Julien Scesa, Janitha Reetz
PMID20231096
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, compounds from this series have favorable rat pharmacokinetic properties suitable for in vivo efficacy evaluation.