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Molecules 2017, 22(6), 773;

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

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
School of Pharmaceutical Sciences, Sun Yat-sen University, 132 Waihuan East Road, Guangzhou 510006, China
The authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editors: Grzegorz Wegrzyn, Luciano Saso, László Dux and Tamás Csont
Received: 18 March 2017 / Revised: 22 April 2017 / Accepted: 27 April 2017 / Published: 1 June 2017
(This article belongs to the Special Issue Chemistry and Pharmacology of Modulators of Oxidative Stress)
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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. View Full-Text
Keywords: isothiocyanate; anticancer; reactive oxygen species; glutathione isothiocyanate; anticancer; reactive oxygen species; glutathione

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Luo, B.; Wang, J.; Li, X.; Lu, W.; Yang, J.; Hu, Y.; Huang, P.; Wen, S. New Mild and Simple Approach to Isothiocyanates: A Class of Potent Anticancer Agents. Molecules 2017, 22, 773.

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