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.

中文翻译：

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鉴定4-（2-呋喃基）嘧啶-2-胺为Janus激酶2抑制剂

Janus激酶抑制剂被认为具有治疗肿瘤和免疫炎性疾病的治疗潜力。设计了两个系列的4-（2-苯并呋喃基）嘧啶-2-胺和4-（4,5,6,7-四氢呋喃[3,2-c]吡啶-2-基）嘧啶-2-胺衍生物并合成。初步的SAR研究导致发现了一种新型的4,5,6,7-四氢呋喃[3,2-c]吡啶基的JAK2抑制剂，具有更高的效力（IC ₅₀为0.7nM）和选择性（> 30倍）比托法替尼对JAK3激酶的作用更大。