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

oleh: 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

Format: Article
Diterbitkan: MDPI AG 2012-08-01

Deskripsi

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).