Related Experiment Video
Updated: Mar 13, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors
Yazhou Wang1, Wei Huang1, Minhang Xin2
1Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, PR China; Jiangsu Simcere Pharmaceutical Co. Ltd, Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, No 699-18, Xuan Wu District, Nanjing 210042, PR China.
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.
Related Concept Videos
The JAK-STAT Signaling Pathway
cAMP-dependent Protein Kinase Pathways
PI3K/mTOR/AKT Signaling Pathway
Inhibition of Cdk Activity
Inhibition of CDK Activity
Dipeptidyl Peptidase 4 Inhibitors

