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  • Title: Structure-based design of a novel synthetic spiroketal pyran as a pharmacophore for the marine natural product spongistatin 1.
    Author: Uckun FM, Mao C, Vassilev AO, Huang H, Jan ST.
    Journal: Bioorg Med Chem Lett; 2000 Mar 20; 10(6):541-5. PubMed ID: 10741549.
    Abstract:
    SPIKET-P, a novel synthetic spiroketal pyran, was rationally designed as a pharmocophore for the tubulin depolymerizing marine natural product Spongistatin 1. SPIKET-P was prepared from the commercially available benzyl (R)-(-)-glycidyl ether using a versatile 11-step synthetic scheme in a stereocontrolled fashion. At nanomolar concentrations, SPIKET-P caused tubulin depolymerization in cell-free turbidity assays and exhibited potent cytotoxic activity against cancer cells as evidenced by destruction of microtubule organization, and prevention of mitotic spindle formation in human breast cancer cells.
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