Boron in drug design: Recent advances in the development of new therapeutic agents

Eur J Med Chem. 2019 Oct 1;179:791-804. doi: 10.1016/j.ejmech.2019.06.092. Epub 2019 Jul 3.


Advances in the field of boron chemistry have expanded the application of this element in Medicinal Chemistry. Boron-containing compounds represent a new class for medicinal chemists to use in their drug designs. Bortezomib (Velcade®), a dipeptide boronic acid approved by the FDA in 2003 for treatment of multiple myeloma, paved the way for the discovery of new boron-containing compounds. After its approval, two other boron-containing compounds have been approved, tavaborole (Kerydin®) for the treatment of onychomicosis and crisaborole (Eucrisa®) for the treatment of mild to moderate atopic dermatitis. A number of boron-containing compounds have been described and evaluated for a plethora of therapeutic applications. The present review is intended to highlight the recent advances related to boron-containing compounds and their therapeutic applications. Here, we focused only in those most biologically active compounds with proven in vitro and/or in vivo efficacy in the therapeutic area published in the last years.

Keywords: Benzoxaboroles; Biological activity; Boron; Boron-containing compounds; Boronic acids; Drug design.

Publication types

  • Review

MeSH terms

  • Animals
  • Boron Compounds / chemical synthesis
  • Boron Compounds / chemistry
  • Boron Compounds / therapeutic use*
  • Bortezomib / chemical synthesis
  • Bortezomib / chemistry
  • Bortezomib / therapeutic use*
  • Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis
  • Bridged Bicyclo Compounds, Heterocyclic / chemistry
  • Bridged Bicyclo Compounds, Heterocyclic / therapeutic use*
  • Dermatitis, Atopic / drug therapy*
  • Drug Design
  • Humans
  • Multiple Myeloma / drug therapy*
  • Onychomycosis / drug therapy*


  • Boron Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Bortezomib
  • tavaborole
  • crisaborole