Pharmaceuticals (Feb 2022)

The Boron Advantage: The Evolution and Diversification of Boron’s Applications in Medicinal Chemistry

  • Katia Messner,
  • Billy Vuong,
  • Geoffrey K. Tranmer

DOI
https://doi.org/10.3390/ph15030264
Journal volume & issue
Vol. 15, no. 3
p. 264

Abstract

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In this review, the history of boron’s early use in drugs, and the history of the use of boron functional groups in medicinal chemistry applications are discussed. This includes diazaborines, boronic acids, benzoxaboroles, boron clusters, and carboranes. Furthermore, critical developments from these functional groups are highlighted along with recent developments, which exemplify potential prospects. Lastly, the application of boron in the form of a prodrug, softdrug, and as a nanocarrier are discussed to showcase boron’s emergence into new and exciting fields. Overall, we emphasize the evolution of organoboron therapeutic agents as privileged structures in medicinal chemistry and outline the impact that boron has had on drug discovery and development.

Keywords