ArticlePloS one2022
Repositioning of acefylline as anti-cancer drug: Synthesis, anticancer and computational studies of azomethines derived from acefylline tethered 4-amino-3-mercapto-1,2,4-triazole.
Article in PloS one, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 82 citations in OpenAlex.
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- Comprehensive Experimental and Computational Characterization of a Phenylacetamide-Based Molecule.BioMed research international · 2026Article
- Investigation of Carbonic Anhydrase Inhibition, Antioxidant Properties, and Selective Anticancer Activity of Methyl-Substituted Halogenated and Methoxy Conduritols.BioMed research international · 2026Article
- Chemical Composition, Antioxidant, Enzyme Inhibition and Anticancer Activities: Effects on the Expression of Genes Related to Apoptosis and the Polyamine Pathway and Molecular Docking Analyses ofCurrent issues in molecular biology · 2025Article
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- Synthesis biological evaluation and molecular docking of isatin hybrids as anti-cancer and anti-microbial agents.Journal of enzyme inhibition and medicinal chemistry · 2024Article
- Accessing the synthesis of natural products and their analogues enabled by the Barbier reaction: a review.RSC advances · 2024Review
- Baeyer-Villiger oxidation: a promising tool for the synthesis of natural products: a review.RSC advances · 2024Review
- Assessment of Bitterness in Non-Charged Pharmaceuticals with a Taste Sensor: A Study on Substances with Xanthine Scaffold and Allopurinol.Molecules (Basel, Switzerland) · 2024Article
- Yamaguchi esterification: a key step toward the synthesis of natural products and their analogs-a review.Frontiers in chemistry · 2024Review
- Exploring theophylline-1,2,4-triazole tetheredFrontiers in chemistry · 2024Article
- Computational exploration of acefylline derivatives as MAO-B inhibitors for Parkinson's disease: insights from molecular docking, DFT, ADMET, and molecular dynamics approaches.Frontiers in chemistry · 2024Article
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- Unfolding the Antibacterial Activity and Acetylcholinesterase Inhibition Potential of Benzofuran-Triazole Hybrids: Synthesis, Antibacterial, Acetylcholinesterase Inhibition, and Molecular Docking Studies.Molecules (Basel, Switzerland) · 2023Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Novel azomethines derived from acefylline tethered triazole hybrids (7a-k) have been synthesized and evaluated against human liver cancer cell line (Hep G2) using MTT assay. The synthesized series of azomethines exhibited promising efficacy against liver cancer cell line. Screening of the synthesized series identified compound 7d with the least cell viability value (11.71 ± 0.39%) as the most potent anticancer agent in contrast to the reference drug acefylline (cell viability = 80 ± 3.87%). In this study, the potentials of the novel agents (7a-k) to inhibit liver cancer proteins were assessed. Subsequently, the structure-activity relationship of the potential drug candidates was assessed via ADME/T molecular screening. The cytotoxic potential of these derivatives was also investigated by hemolysis and thrombolysis. Their hemolytic and thrombolytic studies showed that all of these drugs had very low cytotoxicity and moderate clot lysis activity. Compound 7g (0.26% hemolysis) and 7k (52.1% clot lysis) were the least toxic and moderate thrombolytic agents respectively.
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