Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY 11201, USA.
Department of Medicine, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.
Molecules. 2022 Apr 19;27(9):2615. doi: 10.3390/molecules27092615.
A standard goal of medicinal chemists has been to discover efficient and potent drug candidates with specific enzyme-inhibitor abilities. In this regard, boron-based bioactive compounds have provided amphiphilic properties to facilitate interaction with protein targets. Indeed, the spectrum of boron-based entities as drug candidates against many diseases has grown tremendously since the first clinically tested boron-based drug, Velcade. In this review, we collectively represent the current boron-containing drug candidates, boron-containing retinoids, benzoxaboroles, aminoboronic acid, carboranes, and BODIPY, for the treatment of different human diseases.In addition, we also describe the synthesis, key structure-activity relationship, and associated biological activities, such as antimicrobial, antituberculosis, antitumor, antiparasitic, antiprotozoal, anti-inflammatory, antifolate, antidepressant, antiallergic, anesthetic, and anti-Alzheimer's agents, as well as proteasome and lipogenic inhibitors. This compilation could be very useful in the exploration of novel boron-derived compounds against different diseases, with promising efficacy and lesser side effects.
药用化学家的一个标准目标是发现具有特定酶抑制剂能力的高效、强效药物候选物。在这方面，基于硼的生物活性化合物提供了两亲性，以促进与蛋白质靶标的相互作用。事实上，自第一个临床测试的硼基药物 Velcade 以来，作为针对许多疾病的药物候选物的硼基实体的范围已经大大增加。在这篇综述中，我们共同代表了目前含硼的药物候选物、含硼类视黄醇、苯并恶唑硼烷、氨基硼酸、碳硼烷和 BODIPY，用于治疗不同的人类疾病。此外，我们还描述了它们的合成、关键的结构-活性关系以及相关的生物活性，如抗菌、抗结核、抗肿瘤、抗寄生虫、抗原生动物、抗炎、抗叶酸、抗抑郁、抗过敏、麻醉和抗阿尔茨海默病药物，以及蛋白酶体和脂肪生成抑制剂。这一汇编对于探索针对不同疾病的新型硼衍生化合物非常有用，具有有希望的疗效和较少的副作用。
