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

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

Chem Rev

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.

Published: March 2024

AI Article Synopsis

  • Boron-containing compounds (BCC) are crucial in medicine, with five FDA-approved drugs for treating cancer, infections, and skin conditions.
  • * BCCs, like boronic acids and boroles, work by forming reversible covalent bonds with proteins, leveraging boron's Lewis acidity.
  • * The applications of BCCs extend beyond drugs, including use in imaging technologies and potential therapies for neutron capture and diagnostics.

Article 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.

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Source
http://dx.doi.org/10.1021/acs.chemrev.3c00663DOI Listing

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