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◆ Pharmaceuticals2025-11-26· Drug discovery

Recent Advancements in the Diversification and Applications of Boron-Containing Compounds in Medicinal Chemistry

Marielle B. Frooman, Moinak K. Deb, James Caleb Peters Thomas Rathnakumar Peters, Sasha Leggett, Nitesh Sanghai, Nafees Zahra Rizvi, Devi Atukorallaya, Geoffrey K. Tranmer

原始摘要(英文原文)· Original abstract
Boron-containing compounds have made a significant impact on the field of medicinal chemistry since the discovery of Bortezomib (Velcade®), a dipeptide boronic acid approved by the FDA in 2003 for the treatment of multiple myeloma. Since then, over the last two decades, four more boron-containing drugs have been approved by the FDA: Tavaborole (Kerydin®), Ixazomib (Ninlaro®), Crisaborole (Eucrisa®), and Vaborbactam (in Vabomere®). These compounds are approved for treating conditions such as onychomycosis, multiple myeloma, and atopic dermatitis, as well as an Aβ-lactamase inhibitor approved in combination with meropenem for treating infections. Further, many organic molecules containing boron are in clinical trials. Additionally, boron-containing compounds play a crucial role in various biological processes. Boron’s Lewis acidity has been utilized for diverse applications, from targeting biological molecules to the synthesis of organic compounds and in advanced drug delivery systems. Recent progress in the advancement of boron-containing compounds has not stopped, and the further use of Boron is emerging day-by-day with the discovery of multifaceted applications. This review aims to highlight the recent advances made in the last decade in the drug design of boron-containing compounds and their therapeutic applications. Here, in this work, we have focused on the recent diversification and progress of boron-containing compounds in medicinal chemistry applications.
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