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    Camptothecin analogues and methods of preparation thereof
    63.
    发明授权
    Camptothecin analogues and methods of preparation thereof 失效
    喜树碱类似物及其制备方法

    公开(公告)号：US5525731A

    公开(公告)日：1996-06-11

    申请号：US328415

    申请日：1994-10-25

    申请人： Samuel J. Danishefsky ,  Lawrence B. Snyder

    发明人： Samuel J. Danishefsky ,  Lawrence B. Snyder

    IPC分类号： C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07H17/00 ,  A61K31/435

    CPC分类号： C07D491/14 ,  C07H17/00

    摘要： Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, or CN; R.sup.0 and R.sup.1 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl or aryl group; R.sup.2, R.sup.3 and R.sup.4 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl or aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl or aryl group, or an alkoxy, aryloxy, hydroxyalkyl, C-glycal, nitro, cyano or aminoalkoxy group, or CO.sub.2 R, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12 or OR.sup.13 ; R is H, an alkyl, aryl, alkylaryl or hydroxyalkyl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, an alkyl, aryl, alkylaryl or acyl group; R.sup.13 is glycosyl; and n is 0 or 1. Also provided are compositions comprising the analogues and methods of treating tumors as well as methods for preparing the analogues.

    摘要翻译： 具有一般结构的具有对癌细胞的细胞毒性活性的喜树碱的取代类似物：其中E是H，CO 2 R，CONH 2，CONHR，CONR 2或CN; R 0和R 1独立地相同或不同，为H，或直链或支链烷基，直链或支链烷基芳基，羟烷基或芳基; R2，R3和R4独立地相同或不同，为H，或直链或支链烷基，直链或支链烷基芳基，羟基烷基或芳基; R 5，R 6，R 7，R 8和R 9独立地相同或不同，为H，或直链或支链烷基，直链或支链烷基芳基或芳基，或烷氧基，芳氧基，羟基烷基，C-缩醛，硝基，氰基或 氨基烷氧基或CO2R，Cl，F，Br，I，SR10，NR11R12或OR13; R是H，烷基，芳基，烷基芳基或羟烷基; R 10，R 11和R 12独立地相同或不同，为H，烷基，芳基，烷基芳基或酰基; R13是糖基; 并且n为0或1.还提供了包含治疗肿瘤的类似物和方法的组合物以及制备类似物的方法。