{"title":"Ligustrazine as a multitarget scaffold in drug design and discovery","authors":"Xueyang Jiang , Siyi Li , Ning Wang , Jiaming Li","doi":"10.1016/j.bmc.2025.118110","DOIUrl":null,"url":null,"abstract":"<div><div>Ligustrazine has gained significant attention for its unique structural role in natural medicinal chemistry and its potential in drug discovery and development. The ligustrazine structure has been recognized as a clinical drug for treating cardiovascular and cerebrovascular diseases, especially in the design of neuroprotective agents. Recently, ligustrazine-based anti-tumor agents have also been reported. This knowledge can undoubtedly be applied to design multi-target-directed ligands, a highly relevant strategy for the complex pathological conditions of multifactorial diseases. In this review, we first discuss the biological properties and clinical applications of ligustrazine, then focus on the rational design of ligustrazine-based multifunctional ligands.</div></div>","PeriodicalId":255,"journal":{"name":"Bioorganic & Medicinal Chemistry","volume":"121 ","pages":"Article 118110"},"PeriodicalIF":3.3000,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0968089625000513","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Ligustrazine as a multitarget scaffold in drug design and discovery
Ligustrazine has gained significant attention for its unique structural role in natural medicinal chemistry and its potential in drug discovery and development. The ligustrazine structure has been recognized as a clinical drug for treating cardiovascular and cerebrovascular diseases, especially in the design of neuroprotective agents. Recently, ligustrazine-based anti-tumor agents have also been reported. This knowledge can undoubtedly be applied to design multi-target-directed ligands, a highly relevant strategy for the complex pathological conditions of multifactorial diseases. In this review, we first discuss the biological properties and clinical applications of ligustrazine, then focus on the rational design of ligustrazine-based multifunctional ligands.
期刊介绍：
Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides.
The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.
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