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Molecules 2012, 17(9), 10331-10343; doi:10.3390/molecules170910331
Article

Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells

1, 1, 2, 2, 3, 3, 4, 1 and 1,*
Received: 21 June 2012 / Revised: 1 August 2012 / Accepted: 2 August 2012 / Published: 29 August 2012
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Abstract

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).
Keywords: chalcone; cycloaddition; O-alkylation; HeLa cells chalcone; cycloaddition; O-alkylation; HeLa cells
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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da Silva, G.D.; da Silva, M.G.; Souza, E.M.P.V.E.; Barison, A.; Simões, S.C.; Varotti, F.P.; Barbosa, L.A.; Viana, G.H.R.; Villar, J.A.F.P. Design and Synthesis of New Chacones Substituted with Azide/Triazole Groups and Analysis of Their Cytotoxicity Towards HeLa Cells. Molecules 2012, 17, 10331-10343.

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