Cancer is one of the major causes of death worldwide, emphasizing the critical need for safer and more effective anticancer drugs. Heterocyclic scaffolds are important in the development of anticancer drugs due to their structural variety and extensive biological activity; among these, oxadiazole has emerged as a notable pharmacophore with excellent physicochemical features and exceptional therapeutic potential. Oxadiazole-based derivatives have strong anticancer activity against a variety of human cancer cell lines by targeting key molecular pathways such as tubulin polymerization, epidermal growth factor receptor, vascular endothelial growth factor receptor-2, topoisomerases, and histone deacetylases. Furthermore, hybrid compounds incorporating the oxadiazole scaffold have shown improved efficacy, enhanced cancer cell selectivity, and lower toxicity, emphasizing the scaffold’s usefulness in the rational design of innovative anticancer medicines. This study provides a comprehensive summary of recent advances in the design, synthesis, biological evaluation, structure-activity relationships, and molecular docking studies of oxadiazole derivatives as anticancer medicines.
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Jadhav et al. (2026) studied this question.
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