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Synthesis, Molecular Docking, and Biological Evaluation of Pyridin-3-Yl-Pyrimidin-2-Yl-Triazole Derivatives As Anti-Cancer Agents Publisher



Firoozpour L1 ; Moghimi S2 ; Fallah Barzegar MH2 ; Toolabi M3 ; Salarinejad S1 ; Bijanzadeh HR4 ; Sadat Ebrahimi SE1, 2 ; Safari F5 ; Foroumadi A1, 2
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Department of Medicinal Chemistry, International Campus, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Medicinal Chemistry, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
  4. 4. Department of Environmental Sciences, Faculty of Natural Resources and Marine Sciences, Tarbiat Modares University, Tehran, Iran
  5. 5. Department of Biology, Faculty of Science, University of Guilan, Rasht, Iran

Source: Polycyclic Aromatic Compounds Published:2024


Abstract

In this work, novel imatinib-based compounds were synthesized, characterized, and evaluated against, PC3, Panc1, MDA-MB-231, and K562. The synthetic procedure was started from methyl-4-hydroxy benzoate and afforded the desired compounds through six steps. Among synthesized compounds, N-(4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((1-(2-((4-methyl-3-nitrophenyl)amino)-2-oxoethyl)-1H-1,2,3-triazol-4-yl)methoxy)benzamide, 11q was found effective against cancer cell lines. Interestingly, the activity of compound 11q was higher than Imatinib (as the standard control). Besides, three-dimensional cell culture along with DAPI-staining assay was performed to get insight about the mechanism of activity. Molecular docking pointed out that triazole moiety formed hydrogen bond and has an important effect on observed activity. © 2023 Taylor & Francis Group, LLC.
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