Advancement of Imidazole Derivatives as Potential Anticancer Agents: Insight Into Structural Activity Relationship (SAR) Studies

ABSTRACT Cancer is a leading cause of mortality worldwide, with 21 million deaths projected by 2030. Conventional chemotherapy is often constrained by toxicity, lack of specificity, and drug resistance, highlighting the need for safer, more targeted therapies. Imidazole derivatives, a versatile class of heterocyclic compounds, have emerged as potent anticancer agents. They act by inhibiting key signaling pathways, inducing apoptosis, and causing cell cycle arrest in cancer cell lines such as MCF‐7 and MDA‐MB‐231. Structural modifications and metal complexation further enhance their efficacy, with some derivatives demonstrating potency comparable to or exceeding standard chemotherapeutics. These advances position imidazole derivatives as promising candidates for next‐generation cancer therapies, offering selective, effective, and less toxic treatment options. Continued investigation of their structure–activity relationships and underlying mechanisms may accelerate the development of novel, targeted anticancer agents.