Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors |
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| Authors: | Yazhou Wang Wei Huang Minhang Xin Pan Chen Li Gui Xinge Zhao Feng Tang Jia Wang Fei Liu |
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| Affiliation: | 1. Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, PR China;2. Jiangsu Simcere Pharmaceutical Co. Ltd, Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, No 699-18, Xuan Wu District, Nanjing 210042, PR China;3. Department of Medicinal Chemistry, School of Pharmacy, Health Science Center, Xi’an Jiaotong University, No 76, Yanta West Road, Xi’an 710061, PR China |
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| 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 0.7 nM) and selectivity (>30 fold) to JAK3 kinase than tofacitinib. |
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| Keywords: | JAK2 inhibitor 4-(2-Furanyl)pyrimidin-2-amine Kinase selectivity |
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