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色酮作为药物发现中的优势骨架:最新进展

Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances.

作者信息

Reis Joana, Gaspar Alexandra, Milhazes Nuno, Borges Fernanda

机构信息

CIQUP/Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto , Porto 4169-007, Portugal.

出版信息

J Med Chem. 2017 Oct 12;60(19):7941-7957. doi: 10.1021/acs.jmedchem.6b01720. Epub 2017 Jun 13.

Abstract

The use of privileged structures in drug discovery has proven to be an effective strategy, allowing the generation of innovative hits/leads and successful optimization processes. Chromone is recognized as a privileged structure and a useful template for the design of novel compounds with potential pharmacological interest, particularly in the field of neurodegenerative, inflammatory, and infectious diseases as well as diabetes and cancer. This perspective provides the reader with an update of an earlier article entitled "Chromone: A Valid Scaffold in Medicinal Chemistry" ( Chem. Rev. 2014 , 114 , 4960 - 4992 ) and is mainly focused on chromones of biological interest, including those isolated from natural sources. Moreover, as drug repurposing is becoming an attractive drug discovery approach, recent repurposing studies of chromone-based drugs are also reported.

摘要

在药物发现中使用优势结构已被证明是一种有效的策略,能够产生创新的活性化合物/先导化合物,并实现成功的优化过程。色酮被认为是一种优势结构,也是设计具有潜在药理学意义的新型化合物的有用模板,特别是在神经退行性疾病、炎症性疾病、感染性疾病以及糖尿病和癌症领域。这篇综述为读者提供了一篇早期文章《色酮:药物化学中的有效骨架》(《化学评论》2014年,第114卷,4960 - 4992页)的更新内容,主要聚焦于具有生物学意义的色酮,包括从天然来源分离得到的色酮。此外,由于药物重新定位正成为一种有吸引力的药物发现方法,本文还报道了基于色酮药物的近期重新定位研究。

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