Title:Acenaphthotriazine Thio-triazole Derivatives as Anti-cancer Agents
Triggering Cell Cycle Arrest in Breast Cancer Cells
Volume: 20
Issue: 6
Author(s): Aida Iraji, Nasim Shahrokh, Omidreza Firuzi, Maryam Mohabbati, Ramin Miri, Hossein Sadeghpour, Mehdi Khoshneviszadeh*Najmeh Edraki*
Affiliation:
- Medicinal and Natural Products Chemistry Research Center,
Shiraz University of Medical Sciences, Shiraz, Iran
- Department of Medicinal Chemistry, Faculty of Pharmacy,
Shiraz University of Medical Sciences, Shiraz, Iran
- Medicinal and Natural Products Chemistry Research Center,
Shiraz University of Medical Sciences, Shiraz, Iran
Keywords:
Anti-cancer effect, cell cycle, click chemistry, acenaphtho triazine triazole, derivatives, cycloaddition condensation.
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.