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Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury

文献类型：期刊论文

作者Chen, Chao1,2; Lu, Tian2,3; Chen, Panyu4,5; Li, Zizhou2; Yang, Yaxi2,6,8; Fan, Shijie2; Zhang, Yuanyuan4,5; Chen, Kaixian4,8; Fu, Wei1; Wang, Yugang5
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2023-02-05
卷号247页码:13
ISSN号0223-5234
关键词BET Bromodomains Acute liver injury Anti-inflammatory activity Inhibitors Tetracyclic compounds
DOI10.1016/j.ejmech.2022.115023
通讯作者Fu, Wei(wfu@fudan.edu.cn) ; Wang, Yugang(wyg0061@shtrhospital.com) ; Zhou, Bing(zhoubing@simm.ac.cn)
英文摘要Acute liver injury (ALI) is characteristic of abrupt hepatic dysfunction and inflammatory response, and currently the main treatment for ALI is merely supportive rather than curative. Therefore, the development of novel and effective therapeutic strategies for ALI therapy is highly desirable. The emerging biological understanding of the role of BET Bromodomains has opened up an exciting opportunity to develop potent BET Bromodomain inhibitors as an effective therapeutic strategy for the treatment of acute liver injury. Herein, we synthesized a series of potent BET Bromodomain inhibitors with a tetracyclic scaffold, exemplified by compound 28 which showed good in vitro anti-inflammatory activity and good therapeutic effects in the LPS-induced acute liver injury model without obvious cytotoxicity, suggesting that compound 28 is a highly promising candidate worthy for further development.
WOS关键词FAMILY ; BRD4 ; DISCOVERY ; IDENTIFICATION ; CANDIDATE ; PROTEINS ; I-BET151 ; TARGETS
资助项目National Natural Science Foundation of China[81973166] ; Science and Technology Commission of Shanghai Municipality[22XD1424600] ; National Natural Science Foun-dation of China[81973166]
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号WOS:000916315000001
源URL[http://119.78.100.183/handle/2S10ELR8/303579]  
专题新药研究国家重点实验室
通讯作者Fu, Wei; Wang, Yugang; Zhou, Bing
作者单位1.Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, Shanghai 201203, Peoples R China
3.Guizhou Univ Tradit Chinese Med, Guiyang 550025, Guizhou, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Ctr Chem Biol,State Key Lab Drug Res, Shanghai 201203, Peoples R China
5.Shanghai Jiao Tong Univ, Tongren Hosp, Dept Gastroenterol, Sch Med, 1111 XianXia Rd, Shanghai 200336, Peoples R China
6.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
7.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China
8.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Chen, Chao,Lu, Tian,Chen, Panyu,et al. Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2023,247:13.
APA Chen, Chao.,Lu, Tian.,Chen, Panyu.,Li, Zizhou.,Yang, Yaxi.,...&Zhou, Bing.(2023).Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,247,13.
MLA Chen, Chao,et al."Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 247(2023):13.

入库方式： OAI收割

来源：上海药物研究所

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