Biology-Oriented Synthesis of a Tetrahydroisoquinoline-Based Compound Collection Targeting Microtubule Polymerization

Authors

  • Dr. Tobias J. Zimmermann,

    1. Max Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund (Germany)
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    • These authors contributed equally to this work.

  • Dr. Sayantani Roy,

    1. Max Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund (Germany)
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    • These authors contributed equally to this work.

  • Nancy E. Martinez,

    1. Max Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund (Germany)
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  • Dr. Slava Ziegler,

    1. Max Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund (Germany)
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  • Dr. Christian Hedberg,

    1. Max Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund (Germany)
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  • Prof. Dr. Herbert Waldmann

    Corresponding author
    1. Max Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund (Germany)
    2. Faculty of Chemistry, Technical University of Dortmund, Otto-Hahn-Strasse 6,44221 Dortmund (Germany)
    • Max Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund (Germany)
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Abstract

original image

In the third place: Inspired by the tetrahydroisoquinoline (THIQ) alkaloid noscapine, inhibitors of tubulin polymerization that bind to a site different from the colchicine and the vinca alkaloid binding sites have been synthesized. One compound is more potent than noscapine in HeLa cells and can overcome resistance to chemotherapeutics.

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