The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology.

Webster L Santos, Hugo Cerecetto, Ion Romulus Scorei, Clara Viñas, Marvin A Soriano-Ursúa, R Justin Grams, Antonio Abad-García, Carol Ann Rosenblum, Andrei Bita

Journal: Chemical reviews 2024;124(5):2441-2511

PMID: 38382032

Full Text on American Chemical Society View on PubMed

Abstract

Boron-containing compounds (BCC) have emerged as important pharmacophores. To date, five BCC drugs (including boronic acids and boroles) have been approved by the FDA for the treatment of cancer, infections, and atopic dermatitis, while some natural BCC are included in dietary supplements. Boron's Lewis acidity facilitates a mechanism of action via formation of reversible covalent bonds within the active site of target proteins. Boron has also been employed in the development of fluorophores, such as BODIPY for imaging, and in carboranes that are potential neutron capture therapy agents as well as novel agents in diagnostics and therapy. The utility of natural and synthetic BCC has become multifaceted, and the breadth of their applications continues to expand. This review covers the many uses and targets of boron in medicinal chemistry.

Address: Department of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, 900 West Campus Drive, Blacksburg, Virginia 24061, United States.; BioBoron Research Institute, Dunarii 31B Street, 207465 Podari, Romania.; Academia de Fisiología y Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina del Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón s/n, 11340 Mexico City, Mexico.; Department of Pharmacognosy & Phytotherapy, Faculty of Pharmacy, University of Medicine and Pharmacy of Craiova, 2 Petru Rareş Street, 200349 Craiova, Romania.; Centro de Investigaciones Nucleares, Facultad de Ciencias, Universidad de la República, Mataojo 2055, 11400 Montevideo, Uruguay.; Institut de Ciència de Materials de Barcelona (ICMAB-CSIC), Campus UAB, 08193 Bellaterra, Spain.

DOI: 10.1021/acs.chemrev.3c00663

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https://doi.org/10.1021/acs.chemrev.3c00663

MeSH Terms: Humans, Boron, Chemistry, Pharmaceutical, Boron Compounds, Neoplasms, Boronic Acids, Boranes, Boron Neutron Capture Therapy