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

Yazhou Wang, Wei Huang, Minhang Xin, Pan Chen, Li Gui, Xinge Zhao, Feng Tang, Jia Wang, Fei Liu

Bioorganic & medicinal chemistry 2017 Jan 01

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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. Copyright © 2016 Elsevier Ltd. All rights reserved.

Citation

Yazhou Wang, Wei Huang, Minhang Xin, Pan Chen, Li Gui, Xinge Zhao, Feng Tang, Jia Wang, Fei Liu. Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors. Bioorganic & medicinal chemistry. 2017 Jan 01;25(1):75-83