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    2-Indolyl Imidazo [4,5-d] Phenanthroline Derivatives and Their Use in the Treatment for Cancer
    3.
    发明申请
    2-Indolyl Imidazo [4,5-d] Phenanthroline Derivatives and Their Use in the Treatment for Cancer 有权
    2-吲哚咪唑并[4,5-d]菲咯啉衍生物及其在癌症治疗中的应用

    公开(公告)号：US20100168417A1

    公开(公告)日：2010-07-01

    申请号：US11915257

    申请日：2006-05-25

    申请人： Mario Huesca ,  Aiping H. Young ,  Yoon Lee ,  Aye Aye Khine ,  Jim A. Wright ,  Lisa Lock ,  Raed Al-Qawasmeh

    发明人： Mario Huesca ,  Aiping H. Young ,  Yoon Lee ,  Aye Aye Khine ,  Jim A. Wright ,  Lisa Lock ,  Raed Al-Qawasmeh

    IPC分类号： C07D401/14 ,  C07D471/16 ,  C07D413/14

    CPC分类号： C07D471/14

    摘要： 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula I that are capable of intracellular chelation of transition metals and of exerting antiproliferative effects in cancer cells, that are cytostatic and/or cytotoxic, are provided. Compounds of Formula I can also induce apoptosis in cancer cells and are thus capable of exerting a cytotoxic effect on cancer cells. The compounds of Formula I are also capable of selectively inhibiting the proliferation of one or more of prostate cancer cells, colon cancer cells, non-small lung cancer cells and leukemia cells. The compounds of Formula I are also capable of increasing the expression of the zinc-regulated tumour suppressor, KLF4 and thus are useful in inhibiting the proliferation of cancer cells in which KLF4 functions as a tumour-suppressor, including, but not limited to, bladder cancer, cancers of the gastrointestinal tract and various leukemias.

    摘要翻译： 提供能够细胞内螯合过渡金属并且在细胞抑制和/或细胞毒性的癌细胞中发挥抗增殖作用的式I的2-吲哚基咪唑并[4,5-d]菲咯啉化合物。 式I的化合物还可以诱导癌细胞凋亡，因此能够对癌细胞发挥细胞毒性作用。 式I的化合物还能够选择性地抑制一种或多种前列腺癌细胞，结肠癌细胞，非小细胞肺癌细胞和白血病细胞的增殖。 式I的化合物还能够增加锌调节的肿瘤抑制因子KLF4的表达，因此可用于抑制KLF4作为肿瘤抑制剂的癌细胞的增殖，包括但不限于膀胱 癌症，胃肠道癌症和各种白血病。