Boronic Acids and Their Derivatives in Medicinal Chemistry: Synthesis and Biological Applications

Molecules. 2020 Sep 21;25(18):4323. doi: 10.3390/molecules25184323.


Boron containing compounds have not been widely studied in Medicinal Chemistry, mainly due to the idea that this group could confer some toxicity. Nowadays, this concept has been demystified and, especially after the discovery of the drug bortezomib, the interest for these compounds, mainly boronic acids, has been growing. In this review, several activities of boronic acids, such as anticancer, antibacterial, antiviral activity, and even their application as sensors and delivery systems are addressed. The synthetic processes used to obtain these active compounds are also referred. Noteworthy, the molecular modification by the introduction of boronic acid group to bioactive molecules has shown to modify selectivity, physicochemical, and pharmacokinetic characteristics, with the improvement of the already existing activities. Besides, the preparation of compounds with this chemical group is relatively simple and well known. Taking into consideration these findings, this review reinforces the relevance of extending the studies with boronic acids in Medicinal Chemistry, in order to obtain new promising drugs shortly.

Keywords: biological applications; boron-containing compounds; boronic acids; synthesis of boronic acid derivatives.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Boronic Acids / chemical synthesis*
  • Boronic Acids / chemistry
  • Boronic Acids / pharmacology*
  • Chemistry Techniques, Synthetic
  • Humans


  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Antiviral Agents
  • Boronic Acids