Imidazole-based ligands and their transition metal complexes have gained increasing attention in medicinal chemistry owing to their versatile coordination behavior, stability, and wide spectrum of biological activities. Among them, Cu(II), Ag(I), and Au(I) complexes with imidazole derivatives have emerged as promising anti-cancer agents. This review provides a comprehensive overview of recent advances in the design, synthesis, structural features, and biological evaluation of imidazole-based Cu(II), Ag(I), and Au(I) complexes for anti-cancer applications. Special emphasis is placed on their mechanisms of action, including DNA binding and cleavage, apoptosis induction, oxidative stress mediation, enzyme inhibition, and cell cycle arrest. The influence of ligand substitution, geometry, and coordination environment on biological activity is discussed in detail, highlighting structure-activity relationships. Furthermore, the review summarizes in vitro and in vivo studies that demonstrate the therapeutic potential of these complexes against various cancer cell lines. Challenges related to stability, bioavailability, and selectivity are also critically examined, along with future prospects for clinical translation.
Ahmed Abdullah Al Awadh (2026) studied this question.