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    Nitrophenyl, 10-deacetylated substituted taxol derivatives as dual functional cytotoxic/radiosensitizers
    7.
    发明授权
    Nitrophenyl, 10-deacetylated substituted taxol derivatives as dual functional cytotoxic/radiosensitizers 失效
    硝基苯基，10-脱乙酰基取代紫杉醇衍生物作为双功能细胞毒/放射增敏剂

    公开(公告)号：US5780653A

    公开(公告)日：1998-07-14

    申请号：US485496

    申请日：1995-06-07

    申请人： Chunlin Tao ,  Neil P. Desai ,  Patrick Soon-Shiong ,  Paul A. Sandford

    发明人： Chunlin Tao ,  Neil P. Desai ,  Patrick Soon-Shiong ,  Paul A. Sandford

    IPC分类号： A61K41/00 ,  C07D233/91 ,  C07D305/14 ,  C07D305/00 ,  A61K51/04 ,  C07D233/02 ,  C07D413/00

    CPC分类号： C07D305/14 ,  A61K41/0038

    摘要： In accordance with the present invention, there are provided derivatives of chemotherapeutic agents (e.g., paclitaxel), which serve as bifunctional agents. Invention derivatives retain the antitumor activity of the parent compound, and, coupled with the electron affinic substituents thereon, produce compounds which show a strong capability for radiosensitizing tumor cells growing in vitro. It is expected that a single drug which combines the properties of a radiosensitizer with chemotherapeutic activity will offer significant advantages not only to patients, but also to radiotherapists seeking improved modes of treatment. The combination of antitumor properties with electron-affinic function produces novel radiosensitizers, a second generation of drugs which are more powerful to fight cancers. Bifunctional agents with the dual properties of tubulin assembly and electron affinity will make the compounds useful not only as radiosensitizers, but also as cytotoxins.

    摘要翻译： 根据本发明，提供了用作双功能试剂的化学治疗剂（例如紫杉醇）的衍生物。 本发明衍生物保留了母体化合物的抗肿瘤活性，并且与其上的电子亲和取代基一起产生显示出对体外生长的肿瘤细胞放射增敏的强大能力的化合物。 预期将放射增敏剂的性质与化疗活性相结合的单一药物将不仅对患者具有显着的优点，而且还将提供寻求改善治疗方式的放射治疗师的显着优点。 抗肿瘤性质与电子亲和功能的组合产生新型放射增敏剂，第二代更强大的抗癌药物。 具有微管蛋白装配和电子亲和力的双重特性的双功能试剂将使得该化合物不仅用作放射增敏剂，而且用作细胞毒素。