Design and Synthesis of a Series of Novel Macrocycle Janus Kinase 2 Inhibitors

作     者：Yanling Wang Huan Ge Disha Wang Huan He Lu Li Yanyan Diao Zihao Shen Lili Zhu Shiliang Li Zhenjiang Zhao Honglin Li 

作者机构：Shanghai Key Laboratory of New Drug DesignSchool of PharmacyEast China University of Science and Technology130 Meilong RoadShanghai 200237China 

出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)

年 卷 期：2019年第37卷第12期

页      面：1259-1263页

核心收录：

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

基　　金：The research is supported in part by the National Key Research and Development Program(Grant No.2016YFA0502304) the National Natural Science Foundation of China(Grant No.81825020) the National Science&Technology Major Project"Key New Drug Creation and Manufacturing Program",China(No.2018ZX09711002) the Fundamental Research Funds for the Central Universities Honglin Li is also sponsored by the National Program for Special Supports of Eminent Professionals and the National Program for Support of Top-Notch Young Professionals 

主　　题：cycle macrocyclic conclusion 

摘      要：Summary of main observation and conclusion Macrocycle has attracted the attention of many researchers in the field of medicinal chemistry due to its unique advantages and good prospects,but the difficulties in drug design and synthesis of macrocycle limit its *** this study,a series of macrocyclic derivatives designed from anaplastic lymphoma kinase(ALK)inhibitor lorlatinib were synthesized as Janus kinase 2(JAK2)selective *** them,17f had the best inhibitory activity(IC50=0.177μmol·L^-1)and selectivity for JAK2 over JAK1 and JAK3,which indicated that design of the macrocyclic derivatives might be a feasible strategy for the discovery of novel selective JAK2 inhihitors.