Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.

Basic Information

ID: ALA3867460

Journal: Bioorg Med Chem

Title: Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.

Authors: Wang Y, Huang W, Xin M, Chen P, Gui L, Zhao X, Tang F, Wang J, Liu F.

Abstract: Janus kinases inhibitor is considered to have therapeutic potential for the treatment of oncology and immune-inflammatory diseases. Two series of 4-(2-benzofuranyl)pyrimidin-2-amine and 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl)pyrimidin-2-amine derivatives have been designed and synthesized. Primary SAR studies resulted in the discovery of a novel class of 4,5,6,7-tetrahydrofuro[3,2-c]pyridine based JAK2 inhibitors with higher potency (IC50 of 0.7nM) and selectivity (>30 fold) to JAK3 kinase than tofacitinib.

CiteXplore: 27771180

DOI: 10.1016/j.bmc.2016.10.011

Patent ID: ┄