中国药科大学学报2017，Vol.48Issue(5)：554-562,9.DOI:10.11665/j.issn.1000-5048.20170508
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
Design, synthesis and bioactivities of 4-(3-sulfonylbenzene) amino-6-formylpyrrole[2,3-d] pyrimidine derivatives
摘要
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.关键词
磺酰基/吡咯并嘧啶/JAK2抑制剂/合成/生物活性Key words
sulfonyl/pyrrolopyrimidine/JAK2 inhibitors/synthesis/bioactivity分类
医药卫生引用本文复制引用
乔佳男,王庭芳,张灿..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[J].中国药科大学学报,2017,48(5):554-562,9.基金项目
国家自然科学基金资助项目(No.81503003)This study was suported by the National Natural Science Foundation of China (No.81503003) （No.81503003）
