Indole-containing and combretastatin-related anti-mitotic and anti-tubulin polymerization agents
    5.
    发明申请
    Indole-containing and combretastatin-related anti-mitotic and anti-tubulin polymerization agents 审中-公开
    含吲哚和考布他汀相关的抗有丝分裂和抗微管蛋白聚合剂

    公开(公告)号:US20050065217A1

    公开(公告)日:2005-03-24

    申请号:US10861186

    申请日:2004-06-04

    摘要: Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting and destruction chemotherapeutic agents or to have anti-angiogenesis activity resulting in the selective prevention and/or destruction of tumor cell vasculature.

    摘要翻译: 已经发现了三甲氧基苯基取代的吲哚配体,其表现出令人印象深刻的细胞毒性以及抑制微管蛋白聚合的显着能力。 这些化合物以及相关衍生物是用于治疗人类癌症的优异临床候选物。 此外,作为前药的这些配体中的某些可能被证明是肿瘤选择性血管靶向和破坏化学治疗剂,或者具有导致选择性预防和/或破坏肿瘤细胞脉管系统的抗血管生成活性。

    Indole-containing compounds with anti-tubulin and vascular targeting activity
    6.
    发明申请
    Indole-containing compounds with anti-tubulin and vascular targeting activity 审中-公开
    含吲哚的化合物具有抗微管蛋白和血管靶向活性

    公开(公告)号:US20070082872A1

    公开(公告)日:2007-04-12

    申请号:US10555352

    申请日:2004-05-03

    摘要: Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin assembly. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

    摘要翻译: 已经发现了三甲氧基苯基取代的吲哚配体,其表现出令人印象深刻的细胞毒性以及显着的抑制微管蛋白装配的能力。 这些化合物以及相关衍生物是用于治疗人类癌症的优异临床候选物。 此外,作为前药的这些配体中的某些可以很好地证明是肿瘤选择性血管靶向化学治疗剂或具有导致选择性预防和/或破坏非恶性增殖血管的血管靶向活性。