2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2609-13. doi: 10.1016/j.bmcl.2010.02.056.
Carole Pissot-Soldermann 1,  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
Affiliations

Affiliation

  • 1 Novartis Institutes for Biomedical Research, Novartis Pharma AG, WKL-136.4.96, CH-4002 Basel, Switzerland. carole.pissot@novartis.com
PMID: 20231096 DOI: 10.1016/j.bmcl.2010.02.056
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.

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