Recent advances in imidazole-hybrid pharmacophores for anti-cancer applications

Abstract

Cancer is one of the common causes of human death worldwide. There are numerous treatments available nowadays, but chemotherapy is still the leading one. However, it is related to many adverse reactions and causes cancer relapse due to drug resistance. Hence, relay on new potent and less hazardous anti-cancer drugs is still a challenging task for chemists. The imidazole moiety, a class of prominent anti-fungal medications, demonstrates a broad range of biological activity and has been used for cancer treatment. Medicinal chemists are eager to design and synthesize novel imidazole N-heterocyclic-derived molecules because of their high polarity and the tendency to participate in hydrogen bonding and coordination chemistry, enabling them to collaborate with a variety of biomolecules to modulate their bio-efficacy. This review illustrates how the imidazole-hybrid pharmacophores have been used in the recent years to generate cancer-active candidates and stimulate advancements in new cancer-active compounds, using structure-activity correlations, and their future perspectives in anti-cancer drug development are also discussed. © 2025 Elsevier B.V., All rights reserved.