Molecules (Aug 2012)

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

  • José A. F. P. Villar,
  • Gustavo H. R. Viana,
  • Leandro A. Barbosa,
  • Fernando P. Varotti,
  • Sarah C. Simões,
  • Andersson Barison,
  • Estrela M. P. V. E. Souza,
  • Marina G. da Silva,
  • Graziele D. da Silva

DOI
https://doi.org/10.3390/molecules170910331
Journal volume & issue
Vol. 17, no. 9
pp. 10331 – 10343

Abstract

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A series of new chalcones substituted with azide/triazole groups were designed and synthesized, and their cytotoxic activity was evaluated <em>in vitro</em> against the HeLa cell line. <em>O</em>-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 <strong>8c</strong> was the most active molecule, with an IC<sub>50</sub> value of 13.03 µM, similar to the value of cisplatin (7.37 µM).

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