The Cytotoxic Activity of Honokiol-Triazole Derivatives in Ovarian Cancer Cells: The Cytotoxic Activity of Honokiol-Triazole Derivatives

Honokiol-triazole derivatives (4-17) were synthesized via click reactions between 2- or 4 '-propargylated honokiol and azide compounds. Their anticancer activities were evaluated by using two ovarian cancer cells (A2780 and OVCAR3). Among the 14 compounds, compound 5 coupled with 4 '-propargylated honokiol and benzyl azide exhibited relatively potent cytotoxic activity (IC50 = 5.5 +/- 0.5 mu M for A2780 and IC50 = 3.97 +/- 0.6 mu M for OVCAR3) but was less toxic to normal cells (IC50 = 18.90 +/- 0.9 mu M for IOSE80PC). The cytotoxic effect of compound 5 is associated with caspase-dependent apoptotic cell death via induction of intracellular reactive oxygen species.