Discovery of a Novel Benzenesulfonamide Analogue That Inhibits Proliferation and Metastasis Against Ovarian Cancer OVCAR-8 Cells.

BACKGROUND

Ovarian cancer has been a salient public health concern in the world. It is necessary to develop novel antitumor drugs to treat ovarian cancer.

PURPOSE

This study investigated the synthesis, antiproliferation ability, antitumor mechanisms in vitro and in vivo of a novel benzenesulfonamide derivative.

METHODS

The novel benzenesulfonamide-1,2,3-triazole hybrid was synthesized from 4-fluorobenzenesulfonyl chloride, prop-2-yn-1-amine and 1-(azidomethyl)-3-phenoxybenzene. The structure of this benzenesulfonamide-1,2,3-triazole hybrid was confirmed by C NMR, and H NMR. Compound was evaluated for its antitumor effects in vitro and in vivo against ovarian cancer OVCAR-8 cells.

RESULTS

We discovered that the benzenesulfonamide hybrid potently inhibited cell proliferation against ovarian cancer. Especially, it inhibited cell proliferation with an IC value of 0.54μM against OVCAR-8 cells. It could inhibit migration and invasion against OVCAR-8 cells in a concentration-dependent and time-dependent manner. In addition, compound affected the Wnt/β-catenin/GSK3β pathway against ovarian cancer OVCAR-8 cells. In vivo study suggested that compound inhibited tumor growth remarkably without obvious toxicity.

CONCLUSION

In conclusion, benzenesulfonamide hybrid could be a lead compound for further antitumor drug discovery to treat ovarian cancer.