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

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

Molecules. 2017 Jun 01;22(6):

Authors: Luo B, Wang J, Li X, Lu W, Yang J, Hu Y, Huang P, Wen S

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 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.

PMID: 28587167 [PubMed - in process]

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