title: Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.
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.
authors.affiliation: Novartis Institutes for BioMedical Research, Basel, Switzerland. pascal.furet@novartis.com
authors.forename: Pascal
authors.initials: P
authors.lastname: Furet
authors.forename: Marc
authors.initials: M
authors.lastname: Gerspacher
authors.forename: Carole
authors.initials: C
authors.lastname: Pissot-Soldermann
mesh_terms: D015195:Drug Design; D053614:Janus Kinase 2 / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D053614:Janus Kinase 2