Osthole is a natural coumarin-like compound isolated from the Fructus cnidii. In the last few years, this plant-derived product and its derivatives have aroused much attention for their interesting biological activities, including anticancer, anti-inflammatory, neuroprotective, and insecticidal effects. This review summarizes the recent progress on the biological activities of osthole and its derivatives from 2018 to early 2025, with a focus on their total synthesis, structural modifications, and mechanisms of action. Additionally, structure–activity relationships (SARs) of osthole derivatives are presented. This review aims to serve as a comprehensive reference for future research on osthole and its derivatives in both medicinal and agricultural applications.
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