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

被引:12
|
作者
Wen, Xin [1 ]
Wu, Xinyuan [1 ,2 ]
Jin, Rui [1 ]
Lu, Xiaojie [1 ,2 ]
机构
[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
关键词
DNA Encoded library; Drug discovery; Heterocycles; Hit identification; Lead generation; ACTIVITY-RELATIONSHIP SAR; HIGHLY POTENT; IN-VITRO; BIOLOGICAL-ACTIVITIES; BINDING MODE; DISCOVERY; INHIBITORS; TECHNOLOGY; IDENTIFICATION; CHEMISTRY;
D O I
10.1016/j.ejmech.2022.115079
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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.
引用
收藏
页数:26
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