Structure−activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors

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• 作者：Chien-Yu Chen^a ; Chin-Min Lin^a ; ^b ; Hui-Chang Lin^a ; Chien-Fu Huang^c ; Chih-Yu Lee^a ; Tze-Chun Si Tou^a ; Chin-Chuan Hung^a ; ^b ; ^{cc0206hung@gmail.com} ; Chih-Shiang Chang^a ; ^{chihshiang@mail.cmu.edu.tw}
• 关键词：2-Aminobenzofuran ; Multidrug resistance ; MDR ; P-glycoprotein ; P-gp ; ABCB1
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：1023-1035
• 全文大小：1739 K
• 卷排序：125

文摘

Structure–activity relationship of 2-aminobenzofuran scaffold has been established. Compound 43 showed the most potent P-gp inhibitory effect with 11.43 fold at 5 μM. 43 can enhance the sensitization of resistant cell lines toward anticancer agents.