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Synthesis and biological study of a flavone acetic acid analogue containing an azido reporting group designed as a multifunctional binding site probe

  1. Author:
    Malolanarasimhan, K.
    Lai, C. C.
    Kelley, J. A.
    Iaccarino, L.
    Reynolds, D.
    Young, H. A.
    Marquez, V. E.

  2. Author Address

    Frederick Ctr Canc Res, Ctr Canc Res, Lab Med Chem, NCI, Ft Detrick, MD 21702 USA. Ctr Canc Res, Lab Expt Immunol, NCI, Ft Detrick, MD 21702 USA Marquez, VE, Frederick Ctr Canc Res, Ctr Canc Res, Lab Med Chem, NCI, Ft Detrick, MD 21702 USA
    1. Year: 2005
    2. Date: APR 15
  2. Journal: Bioorganic & Medicinal Chemistry
    1. 13
    2. 8
    3. Pages: 2717-2722
  4. Type of Article: Article
  1. Abstract:

    Flavone-8-acetic acid (FAA) is a potent immunomodulatory small molecule that is uniquely characterized as being active on mouse but not human cells. Although FAA is a potent inducer of murine cytokine, chemokine and interferon gene expression, its mode of action remains unknown. In this report, we describe the synthesis of a new flavone acetic acid (FAA) analogue, (2-[2-(4-azidophenyl)-4-oxochromen-8-yl-]acetic acid (compound 2). We demonstrate that compound 2 is equally active as the parent FAA in inducing chemokine gene expression and that the azide functional group is capable of reacting with a reporter molecule, such as the FLAG peptide-phosphine, under mild conditions. This reaction will be useful for detecting the drug-bound protein active complex utilizing an anti-FLAG antibody. Published by Elsevier Ltd

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External Sources

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  2. DOI: 10.1016/j.bmc.2005.02.035
  3. View record in Web of Science®
  4. WOS: 000228254000002

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