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Synthesis and evaluation of piperazine and homopiperazine analogues of JS-K, an anti-cancer lead compound

  1. Author:
    Nandurdikar, R. S.
    Maciag, A. E.
    Citro, M. L.
    Shami, P. J.
    Keefer, L. K.
    Saavedra, J. E.
    Chakrapani, H.

  2. Author Address

    Maciag, Anna E.; Citro, Michael L.; Saavedra, Joseph E.] NCI, Basic Sci Program, SAIC Frederick, Frederick, MD 21702 USA. [Nandurdikar, Rahul S.; Keefer, Larry K.; Chakrapani, Harinath] NCI, Chem Sect, Comparat Carcinogenesis Lab, Frederick, MD 21702 USA. [Shami, Paul J.] Univ Utah, Div Oncol, Dept Internal Med, Salt Lake City, UT 84112 USA.
    1. Year: 2009
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 19
    2. 10
    3. Pages: 2760-2762
  4. Type of Article: Article
  1. Abstract:

    Here we report a number of novel JS-K structural analogues with sub-micromolar anti-proliferative activities against human leukemia cell lines HL-60 and U937, JS-K is the anti-cancer lead compound O-2-(2,4-dinitrophenyl) 1-[(4-ethoxycarbonyl)piperazin-1-yl]diazen-1-ium-1,2-diolate. The ability of these compounds to generate intracellular nitric oxide correlated well with their observed anti-proliferative effects: analogues that had potent inhibitory activity against leukemia cells formed elevated levels of intracellular nitric oxide. (C) 2009 Elsevier Ltd. All rights reserved.

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  2. DOI: 10.1016/j.bmcl.2009.03.115
  3. PMID: 19364650

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