The 1,2,3-triazole ring system has emerged as a versatile scaffold in medicinal chemistry, owing to its remarkable physicochemical stability, hydrogen-bonding potential, and ability to act as a bioisostere. In recent years, its incorporation into anticancer drug design has shown significant promise, particularly in the development of targeted therapies against breast cancer. This review provides a comprehensive overview of the diverse anticancer mechanisms exhibited by 1,2,3-triazole-based compounds, including apoptosis induction, cell cycle arrest, inhibition of kinases and signaling pathways, antiangiogenic and antimetastatic effects, as well as DNA intercalation and topoisomerase inhibition. Special emphasis is placed on their therapeutic relevance in breast cancer, highlighting the structural hybridization of triazoles with pharmacologically active moieties such as coumarins, chalcones, azoles, and other heterocycles. The review further consolidates structure-activity relationship (SAR) trends, identifying key substitutions and linker designs that enhance cytotoxicity and selectivity. By integrating mechanistic insights and SAR data, this article aims to provide a valuable framework for the rational design of next-generation 1,2,3-triazole-based therapeutics in breast cancer treatment. This comprehensive overview aims to support ongoing drug discovery efforts by consolidating key insights into the design and therapeutic potential of 1,2,3-triazole-based hybrids in breast cancer treatment.
Zehra et al. (Fri,) studied this question.