Imine Resveratrol Analogues: Molecular Design, Nrf2 Activation and SAR Analysis
作者： Chang Li , Xiaofei Xu , Xiu Jun Wang , Yuanjiang Pan
DOI: 10.1371/JOURNAL.PONE.0101455
关键词:
摘要: Resveratrol is a natural phenol with protective effects against cancer and inflammation-related diseases. Its mechanism of action involves the activation nuclear factor E2 p45-related 2 (Nrf2), which plays key role in regulation genes driven by antioxidant response element (ARE). Inspired effect resveratrol, here we synthesized series imine resveratrol analogs (IRAs), evaluated their abilities to activate Nrf2 using cell based ARE-reporter assay. After first-round screening, preliminary quantitative structure-activity relationship (SAR) was analyzed, structural features determining ability were proposed. Two novel IRAs designed subsequently synthesized, namely 2-methoxyl-3,6-dihydroxyl-IRA 2,3,6-trihydroxyl-IRA. They proved be most potent activators among IRAs.
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