Boron Chemicals in Drug Discovery and Development: Synthesis and Medicinal Perspective

Bhaskar C. Das, Nitesh K. Nandwana, Sasmita Das, Varsha Nandwana, Mohammed Adil Shareef, Yogarupa Das, Mariko Saito, Louis M. Weiss, Frankis Almaguel, Narayan S. Hosmane, Todd Evans

Research output: Contribution to journalReview articlepeer-review

30 Scopus citations


A standard goal of medicinal chemists has been to discover efficient and potent drug candidates with specific enzyme-inhibitor abilities. In this regard, boron-based bioactive compounds have provided amphiphilic properties to facilitate interaction with protein targets. Indeed, the spectrum of boron-based entities as drug candidates against many diseases has grown tremendously since the first clinically tested boron-based drug, Velcade. In this review, we collectively represent the current boron-containing drug candidates, boron-containing retinoids, benzoxaboroles, aminoboronic acid, carboranes, and BODIPY, for the treatment of different human diseases. In addition, we also describe the synthesis, key structure–activity relationship, and associated biological activities, such as antimicrobial, antituberculosis, antitumor, antiparasitic, antiprotozoal, anti-inflammatory, antifolate, antidepressant, antiallergic, anesthetic, and anti-Alzheimer’s agents, as well as proteasome and lipogenic inhibitors. This compilation could be very useful in the exploration of novel boron-derived compounds against different diseases, with promising efficacy and lesser side effects.

Original languageEnglish (US)
Article number2615
Issue number9
StatePublished - May 1 2022


  • ALS
  • aminoboronic acids
  • bezoxaboroles
  • boron-containing drugs
  • boron-containing retinoids
  • brain cancer
  • lipogenic inhibitors
  • proteasome inhibitors

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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