LAUSR

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.