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The Nitric Oxide Prodrug JS-K and Its Structural Analogues as Cancer Therapeutic Agents

  1. Author:
    Maciag, A. E.
    Saavedra, J. E.
    Chakrapani, H.

  2. Author Address

    Maciag, Anna E.; Saavedra, Joseph E.] NCI, Basic Sci Program, SAIC Frederick, Frederick, MD 21702 USA. [Chakrapani, Harinath] NCI, Chem Sect, Comparat Carcinogenesis Lab, Frederick, MD 21702 USA.
    1. Year: 2009
  2. Journal: Anti-cancer agents in medicinal chemistry
    1. 9
    2. 7
    3. Pages: 798-803
  4. Type of Article: Article
  1. Abstract:

    Nitric oxide (NO) prodrugs of the diazeniumdiolate class are routinely used as reliable sources of nitric oxide in chemical and biological laboratory settings. O-2-(2,4-dinitrophenyl) diazeniumdiolates, which are derivatized forms of ionic diazeniumdiolates, have been found to show potent anti-proliferative activity in a variety of cancer cells, presumably through the effects of NO. One important member of this class of diazeniumdiolates, O-2-(2,4-dinitrophenyl) 1-[(4-ethoxycarbonyl)piperazin-1-yl]diazen-1-ium-1,2-diolate (JS-K), has shown promise as a novel cancer therapeutic agent in a number of animal models. This review describes the developments in chemical and biochemical characterization and structure-activity relationship of JS-K and its analogues. In addition, some molecular mechanistic insights into the observed anti-proliferative activity of JS-K are discussed. Finally, a structural motif is presented for O-2-(aryl) diazeniumdiolate nitric oxide prodrugs that show potency comparable with that of JS-K.

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External Sources

  1. PMID: 19538173

Library Notes

  1. No notes added.
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