Design, synthesis and bioactivities of 4-(3-sulfonylbenzene)amino-6-formylpyrrole［2, 3-d］ pyrimidine derivatives

Taking JAK2 inhibitor baricitinib and fedratinib as the lead compounds, to design the novel 4-(3-sulfonylbenzene)amino-6-formylpyrrole［2, 3-d］ pyrimidine JAK2 inhibitors nucleus using the molecular hybrid drug design principle. 17 target compounds were synthesized by derivatization of sulfonyl and formyl groups respectively. We used JAK2 kinase and GM-CSF-induced TF-1 cells to measure the activities of compounds. The results showed that most compounds had JAK2 inhibitory activities. Among them, compound 31 had excellent inhibitory activity on JAK2 kinase( IC₅₀=0. 009 μmol/L )and GM-CSF-induced TF-1 cells(IC₅₀=0. 136 μmol/L), which proved that the compound had potential research and development value.