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The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology
Chemical Reviews ( IF 51.4 ) Pub Date : 2024-02-21 , DOI: 10.1021/acs.chemrev.3c00663
R Justin Grams 1 , Webster L Santos 1 , Ion Romulus Scorei 2 , Antonio Abad-García 3 , Carol Ann Rosenblum 1 , Andrei Bita 4 , Hugo Cerecetto 5 , Clara Viñas 6 , Marvin A Soriano-Ursúa 3
Affiliation  

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.

中文翻译:


含硼化合物的兴起:合成、药物化学和新兴药理学的进展



含硼化合物(BCC)已成为重要的药效团。迄今为止,FDA 已批准五种 BCC 药物(包括硼酸和硼酸)用于治疗癌症、感染和特应性皮炎,而一些天然 BCC 也包含在膳食补充剂中。硼的路易斯酸性通过在靶蛋白活性位点内形成可逆共价键来促进作用机制。硼还被用于开发荧光团,例如用于成像的 BODIPY,以及碳硼烷,碳硼烷是潜在的中子捕获治疗剂以及诊断和治疗中的新型药物。天然和合成 BCC 的用途已变得多方面,并且其应用范围不断扩大。这篇综述涵盖了硼在药物化学中的许多用途和目标。
更新日期:2024-02-21
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