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Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization

文献类型：期刊论文

作者Wen, Xin1; Wu, Xinyuan1,2; Jin, Rui1; Lu, Xiaojie1,2
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2023-02-15
卷号248页码:26
关键词DNA Encoded library Drug discovery Heterocycles Hit identification Lead generation
ISSN号0223-5234
DOI10.1016/j.ejmech.2022.115079
通讯作者Lu, Xiaojie(xjlu@simm.ac.cn)
英文摘要It is well known that heterocyclic compounds play a key role in improving drug activity, target selectivity, physicochemical properties as well as reducing toxicity. In this review, we summarized the representative het-erocyclic structures involved in hit compounds which were obtained from DNA-encoded library from 2013 to 2021. In some examples, the state of the art in heterocycle-based DEL synthesis and hit-to-lead optimization are highlighted. We hope that more and more novel heterocycle-based DEL toolboxes and in-depth pharmaceutical research on these lead compounds can be developed to accelerate the discovery of new drugs.
WOS关键词ACTIVITY-RELATIONSHIP SAR ; HIGHLY POTENT ; IN-VITRO ; BIOLOGICAL-ACTIVITIES ; BINDING MODE ; DISCOVERY ; INHIBITORS ; TECHNOLOGY ; IDENTIFICATION ; CHEMISTRY
资助项目Shanghai Municipal Science and Technology Major Project[NSFC-91953203] ; Shanghai Municipal Science and Technology Major Project[NSFC-21877117]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000924520600001
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/303373]  
专题新药研究国家重点实验室
通讯作者Lu, Xiaojie
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 501 Haike Rd,Zhang Jiang Hitech Pk, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Wen, Xin,Wu, Xinyuan,Jin, Rui,et al. Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2023,248:26.
APA Wen, Xin,Wu, Xinyuan,Jin, Rui,&Lu, Xiaojie.(2023).Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,248,26.
MLA Wen, Xin,et al."Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 248(2023):26.

入库方式： OAI收割

来源：上海药物研究所

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