Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation

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• 作者：Jinlei Bian^a ; ¹ ; Xiang Li^a ; ¹ ; Lili Xu^a ; Nan Wang^a ; Xue Qian^a ; Qidong You^a ; ^{youqd@163.com} ; Xiaojin Zhang^a ; ^b ; ^{zxj@cpu.edu.cn}
• 关键词：Fluorescent probe ; NQO1 ; Inhibitor ; FITC ; Dicoumarol
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：828-839
• 全文大小：2724 K
• 卷排序：127

文摘

A series inhibitors of NQO1 are designed, synthesized and evaluated. The most potent compound 3d is employed as the recognition group of probe. The first functional affinity-based small-molecule probe for NQO1 is developed. Preliminary biological results demonstrated probe III is favorable for mechanistic studies and cancer diagnostic biomarker.