The Future of Boron in Medicinal Chemistry: Therapeutic and Diagnostic Applications
The Future of Boron in Medicinal Chemistry: Therapeutic and Diagnostic Applications
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DOI：
10.1007/7355_2014_65
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发表时间：
2016-01-01
期刊：
影响因子：
--
通讯作者：
Wang, Binghe
中科院分区：
文献类型：
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作者：
Draganov, Alexander;Wang, Danzhu;Wang, Binghe
由于其独特的电子结构，硼具有可用于设计新的诊断和治疗剂的特殊性质。具体而言，硼的强路易斯酸性和在中子轰击下进行裂变的能力构成了含硼化合物被开发为水解酶抑制剂、碳水化合物和其他路易斯碱的化学传感器和人工受体以及硼中子捕获剂的基础。已在动物和人类研究中评估了许多含硼化合物的诊断和治疗应用。尤其是一种化合物 Velcade，已被批准作为抗癌剂。本章重点介绍了该领域的一些最重要的贡献。
Because of its unique electronic structure, boron has special properties useful in designing new diagnostic and therapeutic agents. Specifically, boron's strong Lewis acidity and ability to undergo fission under neutron bombardment form the foundation for boron-containing compounds to be developed as inhibitors of hydrolytic enzymes, chemosensors and artificial receptors for carbohydrates and other Lewis bases, and boron neutron capture agents. A number of boron-containing compounds have been evaluated in animal and human studies for diagnostics and therapeutic applications. One compound in particular, Velcade, has been approved as an anticancer agent. This chapter highlights some of the most significant contributions in the field.