Abstract
Background: Cancer is one of the most devastating diseases, affecting the lives of millions of people around the world.
Introduction: A series of acenaphtho[1,2-e][1,2,4]triazine containing different thiomethyl-1,2,3-triazole derivatives were designed based on a fragment-based and molecular hybridization approach as anti-cancer agents.
Methods: Designed compounds were synthesized using cycloaddition condensation followed by click reaction. Cytotoxicity of prepared compounds was evaluated by MTT reduction assay against four different cancer cell lines.
Results: The biological evaluation indicated that derivative 6d with para-fluorobenzyl moiety was the most active cytotoxic agent with IC50 values of 70.1, 12.8, 41.5, and 16.0 μM against K562, MOLT-4, HT-29, and MCF-7 cells, respectively. Cell cycle analysis showed that acenaphtho triazine derivatives could induce G0/G1 phase arrest in MCF-7 breast cancer cells.
Conclusion: Synthesized derivatives can be ideal candidates for further exploration as anti-cancer agents.
Keywords: Anti-cancer effect, cell cycle, click chemistry, acenaphtho triazine triazole, derivatives, cycloaddition condensation.
Graphical Abstract
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