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

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机构： [1]Sun Yat Sen Univ, Canc Ctr, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [2]Sun Yat Sen Univ, State Key Lab Oncol South China, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [3]Sun Yat Sen Univ, Collaborat Innovat Ctr Canc Med, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [4]Sun Yat Sen Univ, Sch Pharmaceut Sci, 132 Waihuan East Rd, Guangzhou 510006, Guangdong, Peoples R China

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关键词： isothiocyanate anticancer reactive oxygen species glutathione

摘要：

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.

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出版当年[2017]版：

大类 | 3 区化学

小类 | 3 区有机化学

最新[2023]版：

大类 | 2 区化学

小类 | 3 区生化与分子生物学 3 区化学：综合

第一作者：

第一作者机构： [1]Sun Yat Sen Univ, Canc Ctr, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [2]Sun Yat Sen Univ, State Key Lab Oncol South China, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [3]Sun Yat Sen Univ, Collaborat Innovat Ctr Canc Med, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [4]Sun Yat Sen Univ, Sch Pharmaceut Sci, 132 Waihuan East Rd, Guangzhou 510006, Guangdong, Peoples R China

通讯作者：

通讯机构： [1]Sun Yat Sen Univ, Canc Ctr, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [2]Sun Yat Sen Univ, State Key Lab Oncol South China, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [3]Sun Yat Sen Univ, Collaborat Innovat Ctr Canc Med, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China; [4]Sun Yat Sen Univ, Sch Pharmaceut Sci, 132 Waihuan East Rd, Guangzhou 510006, Guangdong, Peoples R China

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