GLOBAL TRENDS IN THE STUDY OF THE PROPERTIES OF 1,2,4-TRIAZOLE DERIVATIVES (LITERATURE REVIEW)

The relevance of studying 1,2,4-triazole derivatives is driven by their broad application potential in the pharmaceutical, agrochemical, and materials science industries. The discovery of new antifungal agents is crucial due to the increasing prevalence of fungal infections and the emergence of drug-resistant strains. 1,2,4-Triazole derivatives have shown promising antifungal activity, and the presented study aimed to design, synthesise, and evaluate the antifungal potential of a series of new 1,2,4-triazole derivatives. Using an efficient programmed arylation technique, a series of compounds was synthesized and tested for their activity against three human breast cancer cell lines: MDA-MB-231, MCF-7, and ZR-75-1, through in vitro growth inhibition assays. At a concentration of 10 µM, the compounds exhibited anticancer activity in the MCF-7 cell line, with one molecule showing the highest efficacy (IC50 = 4.8 µM). Mechanistic studies indicated an increase in pro-apoptotic protein levels in malignant cells along with permeabilization of the outer mitochondrial membrane, hallmark signs of apoptosis. Further investigations into metabolic stability in various liver microsomes revealed favorable pharmacokinetic properties for the compound. For the first time, we have systematically and comprehensively analyzed and summarized global trends and advancements over the past two years in the study of the properties of 1,2,4-triazole derivatives. The necessity and feasibility of further scientific research in this chosen area have been substantiated.

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Publication Details

Journal
Zenodo (CERN European Organization for Nuclear Research)
Published
2024-12-30
DOI
https://doi.org/10.5281/zenodo.14576638
Primary Topic
Click Chemistry and Applications
Type
article
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article

GLOBAL TRENDS IN THE STUDY OF THE PROPERTIES OF 1,2,4-TRIAZOLE DERIVATIVES (LITERATURE REVIEW)

Zenodo (CERN European Organization for Nuclear Research)
Click Chemistry and Applications
article

GLOBAL TRENDS IN THE STUDY OF THE PROPERTIES OF 1,2,4-TRIAZOLE DERIVATIVES (LITERATURE REVIEW)

article en

Abstract

The relevance of studying 1,2,4-triazole derivatives is driven by their broad application potential in the pharmaceutical, agrochemical, and materials science industries. The discovery of new antifungal agents is crucial due to the increasing prevalence of fungal infections and the emergence of drug-resistant strains. 1,2,4-Triazole derivatives have shown promising antifungal activity, and the presented study aimed to design, synthesise, and evaluate the antifungal potential of a series of new 1,2,4-triazole derivatives. Using an efficient programmed arylation technique, a series of compounds was synthesized and tested for their activity against three human breast cancer cell lines: MDA-MB-231, MCF-7, and ZR-75-1, through in vitro growth inhibition assays. At a concentration of 10 µM, the compounds exhibited anticancer activity in the MCF-7 cell line, with one molecule showing the highest efficacy (IC50 = 4.8 µM). Mechanistic studies indicated an increase in pro-apoptotic protein levels in malignant cells along with permeabilization of the outer mitochondrial membrane, hallmark signs of apoptosis. Further investigations into metabolic stability in various liver microsomes revealed favorable pharmacokinetic properties for the compound. For the first time, we have systematically and comprehensively analyzed and summarized global trends and advancements over the past two years in the study of the properties of 1,2,4-triazole derivatives. The necessity and feasibility of further scientific research in this chosen area have been substantiated.

Zenodo (CERN European Organization for Nuclear Research)
Petro Mohyla Black Sea National University (UA), Zaporizhzhia State Medical and Pharmaceutical University (UA)
Openalex Percentile: Top 70%
Click Chemistry and Applications
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