3-Aroylmethylene-2, 3, 6, 7-tetrahydro-1 H-pyrazino [2, 1-a] isoquinolin-4 (11b H)-ones as Potent Nrf2/ARE Inducers in Human Cancer Cells and AOM-DSS Treated …

M Xi, J Jia, H Sun, Z Sun, J Jiang, Y Wang…

文献索引：Xi, Mei-Yang; Jia, Jian-Min; Sun, Hao-Peng; Sun, Zhong-Ying; Jiang, Jie-Wei; Wang, Ya-Jing; Zhang, Min-Ye; Zhu, Jun-Feng; Xu, Li-Li; Jiang, Zheng-Yu; Xue, Xin; Ye, Ming; Yang, Xi; Gao, Yuan; Tao, Lei; Guo, Xiao-Ke; Xu, Xiao-Li; Guo, Qing-Long; Zhang, Xiao-Jin; Hu, Rong; You, Qi-Dong Journal of Medicinal Chemistry, 2013 , vol. 56, # 20 p. 7925 - 7938

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被引用次数: 12

摘要

Nrf2-mediated activation of ARE regulates expression of cytoprotective enzymes against oxidative stress, inflammation, and carcinogenesis. We have discovered a novel structure (1) as an ARE inducer via luciferase reporter assay to screen the in-house database of our laboratory. The potency of 1 was evaluated by the expression of NQO-1, HO-1, and nuclear translocation of Nrf2 in HCT116 cells. In vivo potency of 1 was studied using AOM-DSS ...