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 7c 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 7c was confirmed by 13C NMR, and 1H NMR. Compound 7c was evaluated for its antitumor effects in vitro and in vivo against ovarian cancer OVCAR-8 cells.

RESULTS

We discovered that the benzenesulfonamide hybrid 7c potently inhibited cell proliferation against ovarian cancer. Especially, it inhibited cell proliferation with an IC50 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 7c affected the Wnt/β-catenin/GSK3β pathway against ovarian cancer OVCAR-8 cells. In vivo study suggested that compound 7c inhibited tumor growth remarkably without obvious toxicity.

CONCLUSION

In conclusion, benzenesulfonamide hybrid 7c could be a lead compound for further antitumor drug discovery to treat ovarian cancer.