Indole-containing and combretastatin-related anti-mitotic and anti-tubulin polymerization agents
申请人:Pinney G. Kevin
公开号:US20050065217A1
公开(公告)日:2005-03-24
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.
已经发现了替甲氧苯基取代的吲哚配体,它们展示出令人印象深刻的细胞毒性以及抑制微管聚合的显着能力。这些化合物以及相关衍生物是治疗人类癌症的优秀临床候选药物。此外,其中某些配体作为前药,可能被证明是肿瘤选择性靶向血管破坏化学治疗药物,或具有抗血管生成活性,从而选择性地预防和/或破坏肿瘤细胞血管。