Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy

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• 作者：Hai-Bo Wang ; Xiao-Ling Jin ; Jia-Fang Zheng ; Fu Wang ; Fang Dai ; Bo Zhou ; ^{bozhou@lzu.edu.cn}
• 关键词：Glutathione S-transferases ; Piperlongumine ; Electrophilicity ; Multiple drug resistance
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：517-525
• 全文大小：2197 K
• 卷排序：126

文摘

Developing GST inhibitors by an electrophilicity-based strategy. A novel analog of piperlongumine (PL-13) as a GST inhibitor was synthesized. PL-13 displayed the strongest electrophilicity and GST-inhibitory activity. PL-13 could effectively overcome cisplatin resistance in lung cancer A549 cells.