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Natural products (NPs) have long served as a rich inspirational source for drug discovery and development, offering diverse chemical structures and biological activities. Among these, topsentin, a marine alkaloid derived from marine sponges, has emerged as a promising scaffold due to its remarkable pharmacological properties and structural versatility. This review explores the significance of topsentin and its derivatives in drug discovery efforts. It discusses the diverse biological activities of topsentin and its analogs, including anticancer, antimicrobial, anti-inflammatory, and antiviral properties, highlighting their potential therapeutic applications. Moreover, it also focuses on the structural features of topsentin that contribute to its pharmacological profile, emphasizing its importance in the design and development of novel therapeutic agents. Structural modifications and synthetic strategies employed to enhance the pharmacological properties of topsentin derivatives are also discussed. Overall, this review underscores the significance of topsentin as a promising scaffold in drug discovery.
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