Design, synthesis and bioactivities of 4-(3-sulfonylbenzene) amino-6-formylpyrrole2,3-d pyrimidine derivatives
10.11665/j.issn.1000-5048.20170508
- VernacularTitle:4-(3-磺酰基苯基)氨基-6-甲酰基吡咯并[2,3-d]嘧啶类化合物的设计、合成与生物活性
- Author:
Jianan QIAO
1
;
Tingfang WANG
;
Can ZHANG
Author Information
1. 中国药科大学新药研究中心
- Keywords:
sulfonyl;
pyrrolopyrimidine;
JAK2 inhibitors;
synthesis;
bioactivity
- From:
Journal of China Pharmaceutical University
2017;48(5):554-562
- CountryChina
- Language:Chinese
-
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.
