{"title":"Coumarin derivatives as HIV-1 inhibitors: mechanistic insights and structure-activity relationships","authors":"Xiaohui Lin, Xijun Sheng, Hao Zhou, Xiongbin Xu, Luanyuan Tian, Shuangxi Gu","doi":"10.1007/s00044-026-03573-y","DOIUrl":null,"url":null,"abstract":"<div><p>Coumarin is a versatile scaffold occurring extensively in abundant natural compounds and synthetic pharmaceuticals. Coumarin derivatives have been proven to inhibit multiple stages of HIV-1 replication, and their unique structures enable them to interact with diverse targets involved in the HIV-1 replication cycle, thereby exerting potent antiviral activity. Currently, HIV-1 inhibitors with novel structures and mechanisms are in urgent need to overcome the existing challenges of drug resistance, safety, and efficacy. Based on the characteristics of the retroviral life cycle, this paper reviews the research progress of coumarin derivatives over the past two decades, aiming to provide valuable insights into the structure-activity relationships (SARs) and design strategies for novel coumarin-based HIV-1 inhibitors in the future.</p></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"35 6","pages":"1064 - 1087"},"PeriodicalIF":3.5000,"publicationDate":"2026-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicinal Chemistry Research","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s00044-026-03573-y","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Coumarin is a versatile scaffold occurring extensively in abundant natural compounds and synthetic pharmaceuticals. Coumarin derivatives have been proven to inhibit multiple stages of HIV-1 replication, and their unique structures enable them to interact with diverse targets involved in the HIV-1 replication cycle, thereby exerting potent antiviral activity. Currently, HIV-1 inhibitors with novel structures and mechanisms are in urgent need to overcome the existing challenges of drug resistance, safety, and efficacy. Based on the characteristics of the retroviral life cycle, this paper reviews the research progress of coumarin derivatives over the past two decades, aiming to provide valuable insights into the structure-activity relationships (SARs) and design strategies for novel coumarin-based HIV-1 inhibitors in the future.
期刊介绍：
Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
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