Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing

Pascal Furet; Marc Gerspacher; Carole Pissot-Soldermann

doi:10.1016/j.bmcl.2010.01.151

Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1858-60. doi: 10.1016/j.bmcl.2010.01.151. Epub 2010 Feb 4.

Authors

Pascal Furet¹, Marc Gerspacher, Carole Pissot-Soldermann

Affiliation

¹ Novartis Institutes for BioMedical Research, Basel, Switzerland. pascal.furet@novartis.com

PMID: 20172718
DOI: 10.1016/j.bmcl.2010.01.151

Abstract

JAK2 is a target of high interest in chronic myeloproliferative disorders drug research. Starting from a screening hit, two new JAK2 inhibitor chemotypes were designed by scaffold morphing. The prototype compounds of these new series showed nanomolar inhibition of the kinase.

MeSH terms

Drug Design
Janus Kinase 2 / antagonists & inhibitors*
Models, Molecular
Protein Kinase Inhibitors / chemical synthesis*
Protein Kinase Inhibitors / pharmacology*

Substances

Protein Kinase Inhibitors
Janus Kinase 2