4.6 Review

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

期刊

MOLECULES
卷 27, 期 9, 页码 -

出版社

MDPI
DOI: 10.3390/molecules27092615

关键词

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

资金

  1. National Institutes of Health [R01AI132614-01A1, R21 AA027374-01, 1R01NS109423-01A1]

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This review introduces current boron-containing drug candidates, including boron-based compounds for the treatment of different diseases. It also describes their synthesis, structure-activity relationship, and associated biological activities.
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.

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