Design and synthesis of new chacones substituted with azide/triazole groups and analysis of their cytotoxicity towards HeLa cells

A series of new chalcones substituted with azide/triazole groups were designed and synthesized, and their cytotoxic activity was evaluated in vitro against the HeLa cell line. O-Alkylation, Claisen-Schmidt condensation and Cu(I)-catalyzed cycloaddition of azides with terminal alkynes were applied in...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2012-08, Vol.17 (9), p.10331-10343
Hauptverfasser:	da Silva, Graziele D, da Silva, Marina G, Souza, Estrela M P V E, Barison, Andersson, Simões, Sarah C, Varotti, Fernando P, Barbosa, Leandro A, Viana, Gustavo H R, Villar, José A F P
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation - drug effects Antiparasitic agents Azide Azides - chemistry Catalysis Cell Death - drug effects Cell Line, Tumor Cell Survival - drug effects Cervical cancer chalcone Chalcones - chemical synthesis Chalcones - chemistry Chalcones - pharmacology Chemotherapy Chromatography cycloaddition Cycloaddition Reaction Cytotoxicity Drug Design Female HeLa Cells Humans Hydrogen bonds Inhibitory Concentration 50 Malaria Molecular Structure O -alkylation Radiation therapy Solvents Triazoles - chemistry
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	A series of new chalcones substituted with azide/triazole groups were designed and synthesized, and their cytotoxic activity was evaluated in vitro against the HeLa cell line. O-Alkylation, Claisen-Schmidt condensation and Cu(I)-catalyzed cycloaddition of azides with terminal alkynes were applied in key steps. Fifteen compounds were tested against HeLa cells. Compound 8c was the most active molecule, with an IC₅₀ value of 13.03 μM, similar to the value of cisplatin (7.37 μM).
ISSN:	1420-3049 1420-3049
DOI:	10.3390/molecules170910331