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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 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.

SUBMITTER: Luo B

PROVIDER: S-EPMC6152774 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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

Luo Bingling B Wang Jiankang J Li Xiaobing X Lu Wenhua W Yang Jing J Hu Yumin Y Huang Peng P Wen Shijun S

Molecules (Basel, Switzerland) 20170601 6

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 toxicit ...[more]

PMID: 28587167

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