<p>Breast cancer continues to represent a major global health burden, driven by its molecular heterogeneity, therapy resistance, and disease recurrence. In recent years, triazole-containing small molecules have gained considerable attention in breast cancer drug discovery owing to their chemical stability, favorable pharmacokinetic properties, and strong ability to engage diverse biological targets. This review focus on the role of triazole scaffolds in breast cancer therapy, covering both clinically approved agents and experimental small molecule inhibitors. FDA-approved triazole-based drugs were discussed to highlight key structure activity relationships and synthetic route that have translated successfully to the clinic. Beyond approved drugs, recent advances in triazole-based inhibitors targeting aromatase, EGFR, VEGFR-2, CDK4/6, BRAF, PARP-1 and dual targets are systematically summarized. Particular focused on representative lead compounds, their reported biological activities, SAR and detailed synthetic routes, along with feasible alternative synthetic strategies that may support future optimization. The ability of triazole moieties to address challenges such as drug resistance, selectivity, and metabolic stability is critically examined. By integrating medicinal chemistry, target biology, and synthetic feasibility, this review aims to provide a practical framework for researchers engaged in the design and development of next-generation triazole-based therapeutics for breast cancer.</p> Graphical abstract <p>Graphical abstract of triazole-based inhibitors targeting breast cancer via key pathways and synthesis strategies.</p> <p></p>