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含单个硼原子化合物的药物化学最新进展。

Recent developments in the medicinal chemistry of single boron atom-containing compounds.

作者信息

Song Shu, Gao Ping, Sun Lin, Kang Dongwei, Kongsted Jacob, Poongavanam Vasanthanathan, Zhan Peng, Liu Xinyong

机构信息

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Ji'nan 250012, China.

Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Odense M. DK-5230, Denmark.

出版信息

Acta Pharm Sin B. 2021 Oct;11(10):3035-3059. doi: 10.1016/j.apsb.2021.01.010. Epub 2021 Jan 20.

Abstract

Various boron-containing drugs have been approved for clinical use over the past two decades, and more are currently in clinical trials. The increasing interest in boron-containing compounds is due to their unique binding properties to biological targets; for example, boron substitution can be used to modulate biological activity, pharmacokinetic properties, and drug resistance. In this perspective, we aim to comprehensively review the current status of boron compounds in drug discovery, focusing especially on progress from 2015 to December 2020. We classify these compounds into groups showing anticancer, antibacterial, antiviral, antiparasitic and other activities, and discuss the biological targets associated with each activity, as well as potential future developments.

摘要

在过去二十年中,多种含硼药物已获批用于临床,目前还有更多药物正处于临床试验阶段。人们对含硼化合物的兴趣与日俱增,这是因为它们对生物靶点具有独特的结合特性;例如,硼取代可用于调节生物活性、药代动力学性质和耐药性。从这一角度出发,我们旨在全面综述硼化合物在药物研发中的现状,特别关注2015年至2020年12月期间的进展。我们将这些化合物分为具有抗癌、抗菌、抗病毒、抗寄生虫及其他活性的几类,并讨论与每种活性相关的生物靶点以及潜在的未来发展方向。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef7e/8546671/a8bd8dc368dd/fx1.jpg

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