Synthesis, Molecular Docking, and Biological Evaluation of Pyridin-3-yl-Pyrimidin-2-yl-Triazole Derivatives as Anti-cancer Agents
- 17 May 2023
- journal article
- research article
- Published by Taylor & Francis Ltd in Polycyclic Aromatic Compounds
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.Keywords
Funding Information
- Tehran University of Medical Sciences (99-1-104-46996)
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