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American Chemical Society, Journal of Medicinal Chemistry, 24(53), p. 8688-8699, 2010

DOI: 10.1021/jm1011066

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Potential Chemopreventive Agents Based on the Structure of the Lead Compound 2-Bromo-1-hydroxyphenazine, Isolated fromStreptomycesSpecies, Strain CNS284

Journal article published in 2010 by Martin Conda-Sheridan, Laura Marler, Eun-Jung Park, Tamara P. Kondratyuk, Katherine Jermihov, Andrew D. Mesecar ORCID, John M. Pezzuto, Ratnakar N. Asolkar, William Fenical ORCID, Mark Cushman
This paper is available in a repository.
This paper is available in a repository.

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Abstract

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.