New Mild and Simple Approach to Isothiocyanates: A Class of Potent Anticancer Agents

Abstract

In our current work, acetyl chloride-mediated synthesis of phenethyl isothiocyanate (PEITC) derivatives proves to be convenient and provides the expected products at good to excellent yields. Biological evaluation and structure-activity relationship analysis found that the novel compound <b>7</b> showed the best anticancer activity against human cancer cell line Panc1 and HGC27 compared with PEITC. Compounds <b>6</b> and <b>7</b> induced more apoptosis in pancreatic cancer cells but less toxicity in non-cancer cells. Further biological study demonstrated that <b>7</b> substantially increased intracellular reactive oxygen species (ROS) and depleted glutathione (GSH), leading to an oxidative stress to kill cancer cell.