2′-Fluorinated nucleoside chemistry for new drug discovery:achievements and prospects  

作　　者：Yonggang Meng Nannan Sun Lan Liang Bin Yu Junbiao Chang 

机构地区：[1]College of Chemistry,Pingyuan Laboratory,State Key Laboratory of Antiviral Drugs,Zhengzhou University,Zhengzhou 450001,China [2]School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001,China [3]State Key Laboratory of Antiviral Drugs,School of Chemistry and Chemical Engineering,Henan Normal University,Xinxiang 453007,China

出　　处：《National Science Review》2024年第10期362-379,共18页国家科学评论（英文版）

基　　金：supported by the National Natural Science Foundation of China(82130103,U1804283,81773570,22277110,82204209,and 82473761);the National Key R&D Program of China(2021YFC0864700 and 2022YFE0202700);the Central Plains Scholars and Scientists Studio Fund(2018002);China Postdoctoral Science Foundation(2023T160601);Henan Province Epidemic Prevention and Control Emergency Research Project(221111311400).

摘　　要：Fluorinated nucleosides are an important class of modified nucleosides that have demonstrated therapeutic potential for treating various human diseases,especially viral infections and cancer.Many fluorinated nucleosides have advanced into clinical trials or have been approved by the FDA for use in patients.Among these fluorinated nucleosides,azvudine,developed by us,has been officially approved by the National Medical Products Administration for the treatment of coronavirus disease 2019(COVID-19)and human immunodeficiency virus,indicating the therapeutic promise of fluorinated nucleosides.In view of the therapeutic promise of fluorinated nucleosides for antiviral and anticancer therapy,in this Review we will provide a comprehensive overview of well-established 2′-fluorinated nucleosides approved for use in the market or those in clinical stages for antiviral and antitumor therapies,highlighting the drug discovery strategies,structure-activity relationship studies,mechanisms of action,and preclinical/clinical studies and also discuss the challenges and future directions for nucleoside-based new drug discovery.

关 键 词：fluorinated nucleosides antitumor activity antiviral activity drug discovery 

分 类 号：R914[医药卫生—药物化学]