Beyond Single-Target Drugs: The Emergence of Dual-Acting Anticancer Molecules

Document Type : Review Articles

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Medicinal Chemistry, Faculty of Pharmacy, Minia University

10.21608/odr.2025.380160.1050

Abstract

Dual-acting anticancer agents represent an innovative and promising strategy in the field of oncology, aiming to overcome the limitations of conventional monotherapies. These compounds are designed to simultaneously target two or more distinct molecular pathways involved in cancer progression, thereby enhancing therapeutic efficacy and reducing the development of drug resistance. By integrating multiple pharmacophores into a single chemical entity, dual-acting agents can exert synergistic effects on crucial biological processes such as cell proliferation, apoptosis, angiogenesis, DNA repair, and immune modulation. In recent years, considerable efforts have been made to design and optimize such agents using rational drug design, structure–activity relationship (SAR) studies, and computational modeling. This review highlights the key mechanisms targeted by dual-acting agents and provides representative examples based on diverse chemical scaffolds, including quinoline, quinazoline, coumarin, triazole, hydantoin, and metal complexes. Furthermore, we discuss the therapeutic potential of these compounds in preclinical and clinical settings, as well as emerging trends in the development of multifunctional drugs. Dual-targeted therapies may represent a transformative approach for improving cancer treatment outcomes and overcoming resistance mechanisms

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