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

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

*Corresponding author for this work

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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.

Original languageEnglish
JournalActa Pharmaceutica Sinica B (Print)
Issue number10
Pages (from-to)3035-3059
Publication statusPublished - Oct 2021


  • Boron-containing compounds
  • Covalent inhibitors
  • Linker components
  • Prodrug


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