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Synthesis and biological evaluation of a spongistatin AB- spiroketal analogue

  1. Author:
    Smith, A. B.
    Corbett, R. M.
    Pettit, G. R.
    Chapuis, J. C.
    Schmidt, J. M.
    Hamel, E.
    Jung, M. K.

  2. Author Address

    Univ Penn, Dept Chem, Philadelphia, PA 19104 USA Univ Penn, Dept Chem, Philadelphia, PA 19104 USA Arizona State Univ, Canc Res Inst, Tempe, AZ 85287 USA NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA NCI, Sci Applicat Int Corp Frederick, NIH, Frederick, MD 21702 USA Smith AB Univ Penn, Dept Chem, Philadelphia, PA 19104 USA
    1. Year: 2002
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 12
    2. 15
    3. Pages: 2039-2042
  4. Type of Article: Article
  1. Abstract:

    The synthesis of a simplified analogue of the potent, cytotoxic tubulin-depolymerizing agent spongistatin 1, based on the AB spiroketal framework, is presented. The new structural analogue is an extension of a recently described spongistatin congener reported to disrupt microtubules in breast cancer cells in vitro and to alter the microtubule assembly reaction. Cytotoxicity data on the new structural analogue, as well as the parent congener, are reported. We found no significant cytotoxic or antitubulin activity with either compound. (C) 2002 Elsevier Science Ltd. All rights reserved.

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