5-(3'-吲哚基)恶唑部分是一种独特的杂环支架，嵌入许多具有生物学意义的天然产物和潜在的治疗剂中。含有这种支架的化合物，无论是天然来源还是合成的，都已表现出广泛的生物活性。这引起了合成化学家的兴趣，导致近年来大量报道了 5-(3'-吲哚基)恶唑支架的合成方法。在这篇综述中，我们全面概述了1963年至2024年文献报道的5-(3'-吲哚基)恶唑支架的不同生物活性和化学合成方法。本研究的重点是强调5-(以3'-吲哚基)恶唑衍生物作为先导化合物，用于抗癌、杀虫、抗菌、抗病毒、抗氧化剂和抗炎药物的先导发现，总结5-(3'-吲哚基)恶唑支架的合成方法。此外，还回顾了已报道的5-(3'-吲哚基)恶唑的作用机制和在动物模型中研究的先进分子。此外，这篇综述还提供了关于未来如何利用 5-(3'-吲哚基)恶唑支架作为一种特殊结构的观点。© 2024 Wiley periodicals LLC。

5-(3'-Indolyl)oxazole moiety is a privileged heterocyclic scaffold, embedded in many biologically interesting natural products and potential therapeutic agents. Compounds containing this scaffold, whether from natural sources or synthesized, have demonstrated a wide array of biological activities. This has piqued the interest of synthetic chemists, leading to a large number of reported synthetic approaches to 5-(3'-indolyl)oxazole scaffold in recent years. In this review, we comprehensively overviewed the different biological activities and chemical synthetic methods for the 5-(3'-indolyl)oxazole scaffold reported in the literatures from 1963 to 2024. The focus of this study is to highlight the significance of 5-(3'-indolyl)oxazole derivatives as the lead compounds for the lead discovery of anticancer, pesticidal, antimicrobial, antiviral, antioxidant and anti-inflammatory agents, to summarize the synthetic methods for the 5-(3'-indolyl)oxazole scaffold. In addition, the reported mechanism of action of 5-(3'-indolyl)oxazoles and advanced molecules studied in animal models are also reviewed. Furthermore, this review offers perspectives on how 5-(3'-indolyl)oxazole scaffold as a privileged structure might be exploited in the future.© 2024 Wiley Periodicals LLC.