2. Academic Validation
  3. Potential chemopreventive agents based on the structure of the lead compound 2-bromo-1-hydroxyphenazine, isolated from Streptomyces species, strain CNS284

Potential chemopreventive agents based on the structure of the lead compound 2-bromo-1-hydroxyphenazine, isolated from Streptomyces species, strain CNS284

  • J Med Chem. 2010 Dec 23;53(24):8688-99. doi: 10.1021/jm1011066.
Martin Conda-Sheridan 1,  Laura Marler,  Eun-Jung Park,  Tamara P Kondratyuk,  Katherine Jermihov,  Andrew D Mesecar,  John M Pezzuto,  Ratnakar N Asolkar,  William Fenical,  Mark Cushman
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and The Purdue University Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, USA.
PMID: 21105712 DOI: 10.1021/jm1011066
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.

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