Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, USA; Department of Medicine and Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.
Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, USA.
Bioorg Med Chem. 2022 Jun 1;63:116748. doi: 10.1016/j.bmc.2022.116748. Epub 2022 Apr 18.
The incorporation of the "magic" boron atom has been established as an important new strategy in the field of medicinal chemistry as boron compounds have been shown to form various bonds with their biological targets. Currently, a number of boron-based drugs (e.g. bortezomib, crisaborole, and tavaborole) have been FDA approved and are in the clinic, and several other boron-containing compounds are in clinical trials. Boron-based heterocycles have an incredible potential in the ongoing quest for new therapeutic agents owing to their plethora of biological activities and useful pharmacokinetic profiles. The present perspective is intended to review the pharmacological applications of boron-based heterocycles that have been published. We have classified these compounds into groups exhibiting shared pharmacological activities and discussed their corresponding biological targets focusing mainly on the most potent therapeutic compounds.
硼原子的引入已被确立为药物化学领域的一项重要新策略,因为硼化合物已被证明可以与生物靶标形成各种键。目前,已有多种基于硼的药物(如硼替佐米、克立硼罗和他泊硼)获得美国食品药品监督管理局批准并在临床上使用,还有其他几种含硼化合物正在临床试验中。基于硼的杂环化合物由于具有丰富的生物活性和有用的药代动力学特性,在寻找新的治疗剂方面具有巨大的潜力。本综述旨在回顾已发表的基于硼的杂环化合物的药理学应用。我们将这些化合物分为具有共同药理活性的组,并讨论了它们相应的生物靶标,主要集中在最有效的治疗化合物上。