A synthetic molecule targeting STAT3 against human oral squamous cell carcinoma cells

Abstract

Oral squamous cell carcinoma (OSCC), one of the most common cancers in Taiwan, needs new therapeutic agents and treatments. The aim of this study was to investigate the anti-proliferative activity of {N-[3-chloro-4-[5-[3-[[[4-[(cyclopropylcarbonyl)-amino]3-(trifluoromethyl)phenylamino]carbonyl]amino]phenyl]-1,2,4-oxadiazol-3-yl]phenyl]-3-pyridine-carboxamide} (COC), a synthetic molecule, in OSCC cells. COC exhibits potent tumor-suppressive efficacy with IC50 values of 195 nM and 204 nM toward SCC2095 and SCC4 OSCC cells, respectively. Our data revealed that COC caused caspase-dependent apoptosis and downregulated the MAPK signaling pathway. In addition, COC modulated the levels of E-cadherin and β-catenin and inhibited migration. COC also decreased p-STAT3 levels, and the overexpression of STAT3 partially attenuated COC-induced cytotoxicity. Therefore, our findings suggest the use of COC as a new approach to oral cancer treatment.