A Water-Soluble Prodrug of Taxol with Self-Assembling Properties

Authors

  • Prof. Dr. Kyriacos Costa Nicolaou,

    Corresponding author
    1. Department of Chemistry, The Scripps Research Institute, 10666 North Torrey Pines Road, La Jolla, CA 92037 (USA)
    2. Department of Chemistry, University of California, San Diego, 9500 Oilman Drive, La Jolla, CA 92093 (USA), Telefax: Int. code + (619)554-6738
    • Department of Chemistry, The Scripps Research Institute, 10666 North Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • Rodney Kiplin Guy,

    1. Department of Chemistry, The Scripps Research Institute, 10666 North Torrey Pines Road, La Jolla, CA 92037 (USA)
    2. Department of Chemistry, University of California, San Diego, 9500 Oilman Drive, La Jolla, CA 92093 (USA), Telefax: Int. code + (619)554-6738
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  • Emmanuel Nicolauo Pitsinos,

    1. Department of Chemistry, The Scripps Research Institute, 10666 North Torrey Pines Road, La Jolla, CA 92037 (USA)
    2. Department of Chemistry, University of California, San Diego, 9500 Oilman Drive, La Jolla, CA 92093 (USA), Telefax: Int. code + (619)554-6738
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  • Wolfgang Wrasidlo

    1. Department of Chemistry, The Scripps Research Institute, 10666 North Torrey Pines Road, La Jolla, CA 92037 (USA)
    2. Department of Chemistry, University of California, San Diego, 9500 Oilman Drive, La Jolla, CA 92093 (USA), Telefax: Int. code + (619)554-6738
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  • This work was supported by the National Institutes of Health, the Office of Naval Research (a predoctoral fellowship to R.K.G.), and The Scripps Research Institute. We thank Drs. R. Milligan and X. Chan for the TEM studies, S. Mauch for the in vivo animal studies, and R. Merlock for development and execution of HPLC and tubulin experiments, Gary Siuzdak for assistance with mass spectrometry, and D.-H. Huang for his help with the NMR studies.

Abstract

original image

Just as effective and not as toxic, taxol derivative 1 displays antitumor activity comparable to that of the parent compound. Since 1 is water soluble, complications that arise in clinical applications of taxol may be avoided.

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