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