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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

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

doi

10.1016/j.bmc.2016.10.011

subject

Has Abstract

pub_date

2017-01-01 00:00:00

pages

75-83

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30926-9

journal_volume

25

pub_type

杂志文章

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