Related Experiment Video
Updated: Aug 5, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Unravelling recent advances in 1,2,4-triazole-based anticancer agents: synthetic strategies, molecular targets,
Glanish Jude Martis1, Eshitha Jane D Souza2, Praveen S Mugali3
1Manipal Institute of Technology, Manipal Academy of Higher Education Manipal India sl.gaonkar@manipal.edu.
Abstract:
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.
Related Concept Videos
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Drugs that Destabilize Microtubules
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Drugs that Stabilize Microtubules
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Drug Discovery: Overview
