Natural and synthetic 5‐(3′‐indolyl)oxazoles: Biological activity, chemical synthesis and advanced molecules

Abstract 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.