Recent Advances in Synthetic Strategies and Medicinal Properties of Thienopyridines

This review provides an updated overview of recent advances (2024–present) in the synthesis and medicinal applications of thienopyridines and their fused derivatives. Synthetic methodologies are categorized into three strategic approaches: (i) thiophene ring construction onto a preformed pyridine core; (ii) pyridine ring annulation onto a thiophene scaffold—ranging from classical Friedländer and Gould–Jacobs reactions to modern metal-catalyzed, photo-induced, and electrochemical transformations; and (iii) multicomponent reactions for the simultaneous assembly of both heterocyclic rings. Furthermore, the strategic functionalization of preformed thienopyridine scaffolds to access complex tri- and polyheterocyclic systems is discussed. From a biological perspective, the review highlights the scaffold’s expanding therapeutic repertoire, including antibacterial, antifungal, and antiviral activities; potent anticancer applications targeting tumor-associated enzymes and emerging Proteolysis Targeting Chimera (PROTAC)/ Deubiquitinase-Targeting Chimera (DUBTAC) technologies; and modulation of neurological, neuropsychiatric, and metabolic disorders. Finally, recent progress in the agrochemical utility of thienopyridines as insecticides and herbicide safeners is examined. Collectively, this work underscores the enduring relevance of the thienopyridine scaffold as a versatile platform for next-generation drug and agrochemical discovery.