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Eur J Med Chem. 2007 Jun;42(6):841-50. Epub 2007 Jan 9.

Quinone reductase induction activity of methoxylated analogues of resveratrol.

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  • 1Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore.

Abstract

Agents that induce the activity of phase II enzymes play an important role in intervening with the carcinogenic process at the initiation stage. Resveratrol is well known for its chemopreventive activity against major stages of carcinogenesis. In this study, several methoxylated analogues of resveratrol were synthesized and evaluated for their ability to induce the activity of the phase II enzyme quinone reductase (QR). Methoxy groups serve to increase lipophilicity and improve metabolic stability. Compared to resveratrol, analogues with ortho-methoxy substituents were found to be more potent inducers of QR and to exert their activity in a qualitatively different manner. The greater induction activities associated with these stilbenoids serve as a useful starting point for the design of improved chemopreventive agents.

PMID:
17316918
DOI:
10.1016/j.ejmech.2006.12.012
[PubMed - indexed for MEDLINE]
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