Unveiling the research directions for pyrrolidine-based small molecules as versatile antidiabetic and anticancer agents.

The pyrrolidine moiety, a five-membered saturated nitrogen-containing heterocycle, emerged as a crucial pharmacophore in medicinal chemistry due to its distinctive physicochemical properties, including hydrophilicity, basicity, and structural rigidity. Extensive modifications of pyrrolidine derivatives yielded novel compounds with pronounced antidiabetic and anticancer activities. The structural investigation of pyrrolidine-based molecules demonstrated that substitutions at the N1, 3^rd, and 5^th positions offer significant opportunities for optimizing biological activity and enhancing target-specific interactions. The synthesis of pyrrolidine-based molecules has been explored in literature; however, structural, target interaction analysis, and pharmacological aspects warranted for the development of targeted small molecule versatile antidiabetic and anticancer agents are lacking. The review addresses this gap by emphasizing the developments in pyrrolidine-based small molecules via structural and target interaction analysis, highlighting their antidiabetic and anticancer activities, and offering a comprehensive perspective on the development of targeted therapeutics. The investigated structural features and pharmacological developments underscore the dual functionality of pyrrolidine-based drugs in managing disorders, such as diabetes and cancer, that share common pathological mechanisms, such as inflammation, oxidative stress, and metabolic dysregulation. This overlap has catalyzed the development of multifunctional pyrrolidine derivatives capable of targeting pathways integral to both conditions, providing a promising avenue for therapeutic innovation.