Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensor Technology and Health, College of Chemistry, Central China Normal University, Wuhan, P. R. China.
Expert Opin Drug Discov. 2020 May;15(5):603-625. doi: 10.1080/17460441.2020.1733526. Epub 2020 Feb 28.
: Spirooxindole, a unique and versatile scaffold, has been widely studied in some fields such as pharmaceutical chemistry and synthetic chemistry. Especially in the application of medicine, quite a few compounds featuring spirooxindole motif have displayed excellent and broad pharmacological activities. Many identified candidate molecules have been used in clinical trials, showing promising prospects.: This article offers an overview of different applications and developments of spirooxindoles (including the related natural products and their derivatives) in the process of drug innovation, including such as in anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, antimalarial, and antiviral activities. Furthermore, the crucial structure-activity relationships, molecular mechanisms, pharmacokinetic properties, and main synthetic methods of spirooxindoles-based derivatives are also reviewed.: Recent progress in the biological activity profiles of spirooxindole derivatives have demonstrated their significant position in present-day drug discovery. Furthermore, we believe that the multidirectional development of novel drugs containing this core scaffold will continue to be the research hotspot in medicinal chemistry in the future.
螺噁吲哚，一种独特且用途广泛的结构骨架，已在药物化学和合成化学等领域得到了广泛研究。特别是在医学应用方面，许多具有螺噁吲哚结构的化合物表现出了优异且广泛的药理活性。许多已鉴定的候选分子已被用于临床试验，显示出了广阔的前景。
本文综述了螺噁吲哚（包括相关天然产物及其衍生物）在药物创新过程中的不同应用和发展，包括在抗癌、抗菌、抗炎、镇痛、抗氧化、抗疟疾和抗病毒活性方面的应用。此外，还综述了螺噁吲哚类衍生物的关键结构-活性关系、分子机制、药代动力学特性和主要合成方法。
螺噁吲哚衍生物的生物活性谱的最新进展表明，它们在当今的药物发现中具有重要地位。此外，我们相信，含有这一核心骨架的新型药物的多方向发展将继续成为未来药物化学的研究热点。
