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Eshitha Jane D. Souza

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Review Open access Jul 2026

Unravelling recent advances in 1,2,4-triazole-based anticancer agents: synthetic strategies, molecular targets, molecular docking studies, and structure–activity relationships

1,2,4-Triazoles have been interesting in the field of heterocyclic chemistry and their utility has been expanded to biological areas including cancer therapy, drug research and development. Thus, this review focuses on the synthetic aspects and biological role played by 1,2,4-triazoles in anticancer treatment and research. Epidermal growth factor receptors (EGFRs), vascular endothelial growth factor-2 (VEGFR-2) and carbonic anhydrases are important classes of oncogenic targets that have attracted significant attention because of their role in cancer studies. By inhibiting these target-specific enzymes it is possible to treat various types of cancer for which 1,2,4-triazoles have shown tremendous progress in development as anticancer agents. Therefore, this review presents recent advances in 1,2,4-triazole chemistry and its biological role in the development of anticancer targets through the inhibition of EGFR, VEGFR-2 and different carbonic anhydrase enzymes. Synthetic aspects help us understand the importance of molecular generation in drug design and discovery. Anticancer studies are helpful for determining the types of active targets among the class of 1,2,4-triazoles. Molecular docking studies reveal major interactions with several amino acid residues and furnish better comparisons with standard reference drugs. A structure–activity relationship (SAR) study enables us to determine the role played by the substituents linked to 1,2,4-triazole hybrids. Herein, we discuss the latest advances in the identification of 1,2,4-triazole-based anticancer targets and active compounds, with the exclusive literature covering the last six years.

Glanish Jude Martis, Eshitha Jane D. Souza, Praveen S. Mugali et al. · 0 citations