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...

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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268421/
https://www.ncbi.nlm.nih.gov/pubmed/22932214
http://dx.doi.org/10.3390/molecules170910331
Descripción
Sumario: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 IC(50) value of 13.03 µM, similar to the value of cisplatin (7.37 µM).

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