imine resveratrol analogues: molecular design, nrf2 activation and sar analysis.

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ID: 166247
2014
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Abstract
Resveratrol is a natural phenol with protective effects against cancer and inflammation-related diseases. Its mechanism of action involves the activation of nuclear factor E2 p45-related factor 2 (Nrf2), which plays a key role in regulation of genes driven by antioxidant response element (ARE). Inspired by the effect of resveratrol, here we synthesized a series of imine resveratrol analogs (IRAs), evaluated their abilities to activate Nrf2 by using cell based ARE-reporter assay. After the first-round screening, preliminary and quantitative structure-activity relationship (SAR) was analyzed, and the structural features determining Nrf2 activation ability were proposed. Two novel IRAs were designed and subsequently synthesized, namely 2-methoxyl-3,6-dihydroxyl-IRA and 2,3,6-trihydroxyl-IRA. They were proved to be the most potent Nrf2 activators among the IRAs.
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li2014plosimine Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Chang Li;Xiaofei Xu;Xiu Jun Wang;Yuanjiang Pan
Journal ensaio pesquisa em educação em ciências
Year 2014
DOI
10.1371/journal.pone.0101455
URL
http://europepmc.org/articles/PMC4100753?pdf=render
Keywords
medicinescience

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