Design, synthesis and bioactivities of 4-(3-sulfonylbenzene) amino-6-formylpyrrole2,3-d pyrimidine derivatives / 中国药科大学学报
Journal of China Pharmaceutical University
;
(6): 554-562, 2017.
Article
in Chinese
| WPRIM
| ID: wpr-664252
ABSTRACT
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of China Pharmaceutical University
Year:
2017
Type:
Article
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