155
Views
0
CrossRef citations to date
0
Altmetric
Research Articles

Synthesis, Molecular Docking, and Biological Evaluation of Pyridin-3-yl-Pyrimidin-2-yl-Triazole Derivatives as Anti-cancer Agents

, , , , , , , & show all
Pages 2062-2076 | Received 09 Nov 2022, Accepted 04 May 2023, Published online: 17 May 2023
 

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.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This work was supported and funded by Tehran University of Medical Sciences, Grant no. 99-1-104-46996.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.