TY - JOUR
T1 - Potential chemopreventive agents based on the structure of the lead compound 2-bromo-1-hydroxyphenazine, isolated from streptomyces species, strain CNS284
AU - Conda-Sheridan, Martin
AU - Marler, Laura
AU - Park, Eun Jung
AU - Kondratyuk, Tamara P.
AU - Jermihov, Katherine
AU - Mesecar, Andrew D.
AU - Pezzuto, John M.
AU - Asolkar, Ratnakar N.
AU - Fenical, William
AU - Cushman, Mark
PY - 2010/12/23
Y1 - 2010/12/23
N2 - The isolation of 2-bromo-1-hydroxyphenazine from a marine Streptomyces species, strain CNS284, and its activity against NF-κB, 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 1 (QR1) and inhibitors of quinone reductase 2 (QR2), NF-κB, 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.
AB - The isolation of 2-bromo-1-hydroxyphenazine from a marine Streptomyces species, strain CNS284, and its activity against NF-κB, 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 1 (QR1) and inhibitors of quinone reductase 2 (QR2), NF-κB, 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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U2 - 10.1021/jm1011066
DO - 10.1021/jm1011066
M3 - Article
C2 - 21105712
AN - SCOPUS:78650354600
SN - 0022-2623
VL - 53
SP - 8688
EP - 8699
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 24
ER -