New Mild and Simple Approach to Isothiocyanates: A Class of Potent Anticancer Agents
Bingling Luo,
Jiankang Wang,
Xiaobing Li,
Wenhua Lu,
Jing Yang,
Yumin Hu,
Peng Huang,
Shijun Wen
Affiliations
Bingling Luo
Sun Yat-Sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer Medicine; Sun Yat-Sen University, 651 Dongfeng East Road, Guangzhou 510060, China
Jiankang Wang
Sun Yat-Sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer Medicine; Sun Yat-Sen University, 651 Dongfeng East Road, Guangzhou 510060, China
Xiaobing Li
Sun Yat-Sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer Medicine; Sun Yat-Sen University, 651 Dongfeng East Road, Guangzhou 510060, China
Wenhua Lu
Sun Yat-Sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer Medicine; Sun Yat-Sen University, 651 Dongfeng East Road, Guangzhou 510060, China
Jing Yang
Sun Yat-Sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer Medicine; Sun Yat-Sen University, 651 Dongfeng East Road, Guangzhou 510060, China
Yumin Hu
Sun Yat-Sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer Medicine; Sun Yat-Sen University, 651 Dongfeng East Road, Guangzhou 510060, China
Peng Huang
Sun Yat-Sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer Medicine; Sun Yat-Sen University, 651 Dongfeng East Road, Guangzhou 510060, China
Shijun Wen
Sun Yat-Sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer Medicine; Sun Yat-Sen University, 651 Dongfeng East Road, Guangzhou 510060, China
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 7 showed the best anticancer activity against human cancer cell line Panc1 and HGC27 compared with PEITC. Compounds 6 and 7 induced more apoptosis in pancreatic cancer cells but less toxicity in non-cancer cells. Further biological study demonstrated that 7 substantially increased intracellular reactive oxygen species (ROS) and depleted glutathione (GSH), leading to an oxidative stress to kill cancer cell.
