Semi-synthesis of β-keto-1,2,3-triazole derivatives from ethinylestradiol and evaluation of the cytotoxic activity.

In this study, we report our contribution to the application of the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction for the synthesis of β-keto-1,2,3-triazole derivatives from ethinylestradiol and their application in the inhibition of two human cancer cells lines: human breast adenocarcinoma (MCF-7) and human hepatocellular carcinoma (HepG2). The β-keto-1,2,3-triazole derivates exhibited moderate cytotoxic activity for the HepG2 cells with IC values of 29.7 μM (), 16.4 μM (), 17.8 μM (), 20.4 μM (), 28.1 μM () and 28.2 μM (). The semi-synthetic β-keto-1,2,3-triazoles derivatives were all characterized by FT-IR, NMR, HRMS and [α].