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    Water soluble analogs and prodrugs of taxol

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    5411984.pdf (1.564Mb)
    Downloads: 282
    Publication Date
    1995-05-02
    Filing Date
    1992-10-16
    Inventor
    Kingston, David G.
    Liang, Jingyu
    Metadata
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    Abstract
    Substituted 2'-benzoyl and 2', 7-dibenzoyl taxol derivatives are synthesized which have improved water solubility and stability while maintaining bioactivity. In a preferred embodiment, taxol 2',7-di(sodium 1,2-benzenedicarboxylate) is synthesized by reacting taxol with phthalic anhydride, and subsequently neutralizing the resulting acid by an ion exchange resin. Taxol 2'-(sodium 1,4-benzenedicarboxylate) is prepared by reacting the monobenzyl ester of 1,4-benzene dicarboxylic acid with taxol in the presence of dicyclohexyl carbodiimide and dimethylaminopyridine, hydrogenolysing the resulting ester to remove the benzyl group, and neutralizing with ion exchange resin. Other taxol prodrugs are prepared by modifications of these routes. In a preferred embodiment, the compounds prepared have improved water-solubility as compared with taxol and demonstrate activity in the M109 mouse bioassay system.
    Assignee
    Virginia Tech Intellectual Properties, Inc.
    Patent Number
    5411984
    Application Number
    7963337
    Source URL
    http://pimg-fpiw.uspto.gov/fdd/84/119/054/0.pdf
    Primary/U.S. Class
    514/449
    Other/U.S. Class
    549/510
    549/511
    CPC Class
    C07D305/14
    Patent Type
    utility
    URI
    http://hdl.handle.net/10919/72833
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