期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 24, 页码 8688-8699出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm1011066
关键词
-
资金
- National Institutes of Health (NIH) [P01 CA48112]
The isolation of 2-bromo-1-hydroxyphenazine from a marine Streptomyces species, strain CNS284, and its activity against NF-kappa B, suggested that a short and flexible route for the synthesis of this metabolite and a variety of phenazine analogues should be developed. Numerous phenazines were subsequently prepared and evaluated as inducers of quinone reductase I (QR1) and inhibitors of quinone reductase 2 (QR2), NF-kappa B, and inducible nitric oxide synthase (iNOS). Several of the active phenazine derivatives displayed IC50 values vs QR1 induction and QR2 inhibition in the nanomolar range, suggesting that they may find utility as cancer chemopreventive agents.
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