典型文献
Design,synthesis and SAR study of 2-aminopyridine derivatives as potent and selective JAK2 inhibitors
文献摘要：
The abnormal activation of JAK2 kinase is closely related to the occurrence and progression of myelo-proliferative neoplasms(MPNs).At present,there is still an obvious unmet medical need for selective JAK2 inhibitors in clinic.In this paper,a class of 2-aminopyridine derivatives as potent and selective JAK2 inhibitors was obtained by combining drug design,synthesis and structure-activity relationship studies based on the previously identified lead Crizotinib.Among them,21b exhibited high inhibitory activity against JAK2 with an IC50 of 9 nmol/L,moreover,it showed 276-and 184-fold selectivity over JAK1 and JAK3,respectively.Besides,21b had a significant antiproliferative activity against HEL cells,and also in-hibited the phosphorylation of JAK2 and its down-stream signaling pathway.These results indicated that 2-aminopyridine compound 21b had the potential to be developed as a selective JAK2 inhibitor for fur-ther study.
文献关键词：
中图分类号：
作者姓名：
Dandan Liu;Huan Ge;Fangling Xu;Yufang Xu;Wenjun Liu;Honglin Li;Lili Zhu;Yanyan Diao;Zhenjiang Zhao
作者机构：
Shanghai Key Laboratory of New Drug Design,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China;Research and Development Department,Jiangzhong Pharmaceutical Co.,Ltd.,Nanchang 330096,China
文献出处：
引用格式：
[1]Dandan Liu;Huan Ge;Fangling Xu;Yufang Xu;Wenjun Liu;Honglin Li;Lili Zhu;Yanyan Diao;Zhenjiang Zhao-.Design,synthesis and SAR study of 2-aminopyridine derivatives as potent and selective JAK2 inhibitors)[J].中国化学快报（英文版）,2022(06):2969-2974
A类：
aminopyridine,myelo,Crizotinib
B类：
Design,synthesis,SAR,study,derivatives,selective,JAK2,inhibitors,abnormal,activation,kinase,closely,related,occurrence,progression,neoplasms,MPNs,At,present,there,still,obvious,unmet,medical,need,clinic,In,this,paper,class,was,obtained,by,combining,drug,design,structure,activity,relationship,studies,previously,identified,lead,Among,them,21b,exhibited,high,inhibitory,against,IC50,nmol,moreover,showed,fold,selectivity,JAK1,JAK3,respectively,Besides,had,significant,antiproliferative,HEL,cells,also,phosphorylation,its,down,stream,signaling,pathway,These,results,indicated,that,compound,potential,be,developed,fur
AB值：
0.577534
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