Design and discovery of boronic acid drugs
Open accessAbstract
Research related to boronic acids, from synthetic development to materials to drug discovery, has skyrocketed in the past 20 years. In terms of drug discovery, the incorporation of boronic acids into medicinal chemistry endeavours has seen a steady increase in recent years. In fact, the Food and Drug Administration (FDA) and Health Canada have thus far approved five boronic acid drugs, three of which were approved in the past four years, and several others are in clinical trials. Boronic acids have several desirable properties that has led to their increased use, including potentially enhancing potency of drugs and/or improving their pharmacokinetics profile. This review explores discovery processes of boronic acid drugs. It begins with a brief scope of boron in natural products and in current drugs, followed by an investigation into the various rationalizations for boronic acid incorporation and the synthetic developments that focused on facilitating their addition into organic compounds. We hope that the knowledge we have assembled in this literature review will encourage medicinal chemists to consider the potential benefits of incorporating boronic acids into their future drug discovery endeavours.
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Several additional boron-containing drugs inhibit serine hydrolases beyond the proteasome by forming covalent adducts between catalytic serine residues and boron.
“Several additional boron-containing drugs inhibit serine hydrolases beyond the proteasome through formation of covalent adducts between catalytic serine residues and boron133,134.”
From Advances in covalent drug discovery (2022) · cites this paper as [134]
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Flagged first, then by citations
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Sorted by citations
Advances in covalent drug discovery
Boike, L., Henning, N. J., & Nomura, D. K. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-022-00542-z · Cited by 823 · see citing works
- Authors
- Plescia, J., & Moitessier, N.
- Affiliations
- McGill University (CA)
- Corresponding author
- Moitessier, Nicolas
- Venue
- European Journal of Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2020-06
- Volume
- 195
- Pages
- 112270
- ISSN
- 0223-5234 (ISSN-L)
- OpenAlex
- W3014843513
- Cited by
- 201
- References
- 145
- Citations by year
- 2026: 25 · 2025: 35 · 2024: 32 · 2023: 27 · 2022: 37 · 2021: 32 · 2020: 13
- FWCI
- 2.19
- Type
- journal article
- Language
- en
- Open access
- Locations
- European Journal of Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- eScholarship@McGill (McGill) (submittedVersion, cc-by)
- Funders
- McGill University
- Canadian Institutes of Health Research (MOP 136943)
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Organoboron and organosilicon chemistry
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Boron Compounds in Chemistry
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Keywords
- boronic acid, drug discovery, boronic acid synthesis, pharmacokinetics, clinical trials
- MeSH terms
- Boronic Acids, Drug Carriers, Humans, Drug Design
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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
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