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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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
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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
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author 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.
author_facet 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.
author_sort da Silva, Graziele D.
collection PubMed
description 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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spelling pubmed-62684212018-12-12 Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells 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. Molecules Article 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). MDPI 2012-08-29 /pmc/articles/PMC6268421/ /pubmed/22932214 http://dx.doi.org/10.3390/molecules170910331 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
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.
Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells
title Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells
title_full Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells
title_fullStr Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells
title_full_unstemmed Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells
title_short Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells
title_sort design and synthesis of new chacones substituted with azide/triazole groups and analysis of their cytotoxicity towards hela cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268421/
https://www.ncbi.nlm.nih.gov/pubmed/22932214
http://dx.doi.org/10.3390/molecules170910331
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