Synthesis of New 1,2,3-Triazolo-naphthalimide/phthalimide Conjugates via ‘Click' Reaction: DNA Intercalation and Cytotoxic Studies
AUTOR(ES)
Shankaraiah, Nagula
FONTE
J. Braz. Chem. Soc.
DATA DE PUBLICAÇÃO
2019-03
RESUMO
Cancer is a complex disease which involves abnormalities of multiple cellular pathways. Current chemotherapeutic drugs are mainly designed to target the DNA and cell division. Therefore, in the present study, we have synthesized a new series of 1,2,3-triazolo-naphthalimide/phthalimide conjugates and evaluated their in vitro cytotoxicity against selected human cancer cells. Among the tested compounds, one of them displayed notable cytotoxic activity against A549 lung cancer cells with an IC50 (half maximal inhibitory concentration) value of 7.6 ± 0.78 µM. To determine the effect of this compound on cell viability, acridine orange/ethidium bromide (AO/EB) and 4',6-diamidino-2-phenylindole (DAPI) staining studies were performed. These apoptotic features were clearly indicating that the compound inhibited cell proliferation by apoptosis. Further, relative viscosity measurements and molecular docking studies with the most three active compounds indicated that these new compounds bind to DNA by intercalation.
Documentos Relacionados
- Combining the Pharmacophore Features of Coumarins and 1,4-Substituted 1,2,3-Triazoles to Design New Acetylcholinesterase Inhibitors: Fast and Easy Generation of 4-Methylcoumarins/1,2,3-triazoles Conjugates via Click Chemistry
- Effect of Sulfamic Acid on 1,3-Dipolar Cycloaddition Reaction: Mechanistic Studies and Synthesis of 4-Aryl-NH-1,2,3-triazoles from Nitroolefins
- Synthesis by Click Reactions and Antiplasmodial Activity of Lupeol 1,2,3-Triazole Derivatives
- Synthesis of new 3-(2-chloroquinolin-3-yl)-5-phenylisoxazole derivatives via click-chemistry approach
- Efficient Eco-Friendly Solvent-Free Click Synthesis and Antimicrobial Evaluation of New Fluorinated 1,2,3-Triazoles and their Conversion into Schiff Bases