利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

3 条记录 (耗时 0.01 秒)

    Carbon-7-substituted atinomycin D analogue
    1.
    发明授权
    Carbon-7-substituted atinomycin D analogue 失效
    碳-7-取代的阿诺霉素D类似物

    公开(公告)号：US4514330A

    公开(公告)日：1985-04-30

    申请号：US508689

    申请日：1983-06-28

    申请人： Sisir K. Sengupta

    发明人： Sisir K. Sengupta

    IPC分类号： A61K38/00 ,  C07K7/06 ,  C07C103/52

    CPC分类号： C07K7/06 ,  A61K38/00 ,  Y10S930/19 ,  Y10S930/27

    摘要： 7-(2,3-Epoxypropoxy)actinomycin D has been synthesized along with its major companion product, 7-(2,3-dihydroxypropoxy)-actinomycin D. They were characterized by UV-visible and CD spectra and by NMR studies. According to UV-visible absorptiometry, circular dichroism, and thermal denaturation studies, they bind to DNA in a manner that is comparable to actinomycin D. The analogues are, like actinomycin D, extremely cytotoxic to human lymphoblastic leukemic cells (CCRF-CEM) in vitro but are significantly less toxic than actinomycin D to normal CDF.sub.1 mice in vivo. Unlike actinomycin, these analogues are metabolized in rats, and the metabolites are excreted in rat urine at a rapid rate. Compared to actinomycin D, the antitumor activity of the 7-(2,3-epoxypropoxy)actinomycin analogue against P-388 leukemia in mice is decidedly superior, and the therapeutic index is improved several fold.

    摘要翻译： 7-（2,3-环氧丙氧基）放线菌素D与其主要伴侣产物7-（2,3-二羟基丙氧基） - 肌动蛋白霉素D一起合成。它们通过紫外可见光谱和CD光谱和NMR研究表征。 根据紫外 - 可见光吸收光谱法，圆二色性和热变性研究，它们以与放线菌素D相当的方式与DNA结合。类似物与放线菌素D类似，对人类淋巴细胞白血病细胞（CCRF-CEM）具有极细胞毒性 体外但与体内正常CDF1小鼠相比，放线菌素D毒性明显更低。 与放线菌素不同，这些类似物在大鼠中代谢，代谢物以大量的尿液排出。 与放线菌素D相比，7-（2,3-环氧丙氧基）放线菌素类似物对小鼠P-388白血病的抗肿瘤活性明显优于治疗指数，改善数倍。

    Method and composition for treating cancer
    2.
    发明授权
    Method and composition for treating cancer 失效
    治疗癌症的方法和组成

    公开(公告)号：US4562176A

    公开(公告)日：1985-12-31

    申请号：US538240

    申请日：1985-10-03

    申请人： Sisir K. Sengupta

    发明人： Sisir K. Sengupta

    IPC分类号： C07K11/00 ,  A61K37/00

    CPC分类号： C07K11/00 ,  Y10S930/19 ,  Y10S930/27

    摘要： Analogues of actinomycin D are provided which are effective in the therapeutic treatment of cancer. The analogues have a 1,4-oxazin-2-one or an oxazole ring or an extra quinone function.

    摘要翻译： 提供放线菌素D的类似物，其有效治疗癌症。 类似物具有1,4-恶嗪-2-酮或恶唑环或额外的醌功能。