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Design, synthesis and biological evaluation of betulinic acid derivatives as potential inhibitors of 3CL-protease of SARS-CoV-2

文献类型：期刊论文

作者Liu, Yaowen1,2; Nie, Tianqing1,4; Hou, Jinjun1,4; Long, Huali1,4; Zhang, Zijia1,4; Lei, Min1,2,3,4; Xu, Yechun1,2,4; Wu, Wanying1,2,3,4
刊名STEROIDS
出版日期2024-02-01
卷号202页码:8
关键词3CLpro SARS-CoV-2 Betulinic acid Natural product Inhibitory activity
ISSN号0039-128X
DOI10.1016/j.steroids.2023.109351
通讯作者Lei, Min(mlei@simm.ac.cn) ; Wu, Wanying(wanyingwu@simm.ac.cn)
英文摘要During the coronavirus reproduction process, 3-chymotrypsin-like protease (3CLpro) and papain-like protease (PLpro) are accountable for the fragmentation of two polyprotein precursors (pp1a/pp1ab) into substructural proteins. These two proteins are vital for the replication and transcription of the viral genome. Therefore, 3CLpro is a key protein and target for the design of coronavirus inhibitors. In previous studies, we found that betulinic acid has an inhibitory effect on 3CLpro, with 51.5 % inhibition of 3CLpro at 20 mu M. Then, series of betulinic acid derivatives were designed, synthesized, and evaluated for their inhibition activities. The results showed that BA02 and BA05 showed significant inhibitory activity on 3CLpro with inhibitory rates of 78.1 % and 82.5 % at 20 mu M, respectively. Further evaluation of these two compounds shows that their IC50 values are 7.22 +/- 0.14 mu M and 6.40 +/- 0.14 mu M, respectively.
WOS研究方向Biochemistry & Molecular Biology ; Endocrinology & Metabolism
语种英语
WOS记录号WOS:001161383200001
出版者ELSEVIER SCIENCE INC
源URL[http://119.78.100.183/handle/2S10ELR8/309228]  
专题中国科学院上海药物研究所
通讯作者Lei, Min; Wu, Wanying
作者单位1.Chinese Acad Sci, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai Inst Mat Med, Natl Engn Lab TCM Standardizat Technol, Shanghai 201203, Peoples R China
2.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, 501 Haike Rd, Shanghai 201203, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Yaowen,Nie, Tianqing,Hou, Jinjun,et al. Design, synthesis and biological evaluation of betulinic acid derivatives as potential inhibitors of 3CL-protease of SARS-CoV-2[J]. STEROIDS,2024,202:8.
APA Liu, Yaowen.,Nie, Tianqing.,Hou, Jinjun.,Long, Huali.,Zhang, Zijia.,...&Wu, Wanying.(2024).Design, synthesis and biological evaluation of betulinic acid derivatives as potential inhibitors of 3CL-protease of SARS-CoV-2.STEROIDS,202,8.
MLA Liu, Yaowen,et al."Design, synthesis and biological evaluation of betulinic acid derivatives as potential inhibitors of 3CL-protease of SARS-CoV-2".STEROIDS 202(2024):8.

入库方式： OAI收割

来源：上海药物研究所

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