Spicamycin derivatives and the use thereof
    23.
    发明授权
    Spicamycin derivatives and the use thereof 失效
    Spicamycin衍生物及其用途

    公开(公告)号:US5631238A

    公开(公告)日:1997-05-20

    申请号:US429303

    申请日:1995-04-26

    CPC分类号: C07H19/16 C07H17/02

    摘要: Disclosed is a novel spicamycin derivative represented by the formula (I) or a salt thereof: ##STR1## wherein R represents an alkenyl having a given number of carbon atoms, a haloalkyl having a given number of carbon atoms, CH.sub.3 (CH.sub.2).sub.n CH(OH)-- or CH.sub.3 (CH.sub.2).sub.n-1 CH(OH)--CH.sub.2 -- (wherein n denotes an integer of 9-13), an alkyl with a certain group and a given number of carbon atoms, ##STR2## (wherein a denotes 2, and b denotes an integer of 10-15), CH.sub.3 (CH.sub.2).sub.c SO.sub.2 O(CH.sub.2).sub.d --, ##STR3## (wherein c denotes an integer of 0-3 and d denotes an integer of 10-15), (CH.sub.3).sub.3 Si(CH.sub.2).sub.10 --,(CH.sub.3).sub.3 Si--C.tbd.C--(CH.sub.2).sub.8 --, ##STR4## (wherein X represents O or S), and R.sub.1 and R.sub.2 are different from each other and each represents H or OH, which exhibits an excellent antitumor effect and has a high therapeutic index.An antitumor agent containing at least one of the above-described compounds in an effective amount is also disclosed.

    摘要翻译: 公开了由式(I)表示的新型的蓖麻霉素衍生物或其盐:其中R表示具有给定数目的碳原子的链烯基,具有给定数目的碳原子的卤代烷基,(CH3)(CH2) )nCH(OH) - 或CH 3(CH 2)n-1 CH(OH)-CH 2 - (其中n表示9-13的整数),具有一定基团和给定数目的碳原子的烷基, (其中a表示2,b表示10-15的整数),CH3(CH2)cSO2O(CH2)d-,其中c表示0-3的整数,d表示 (CH 3)3 Si(CH 2)10 - ,(CH 3)3 Si-C 3BOND C - (CH 2)8 - ,其中X表示O或S) ,R1和R2彼此不同,各自表示H或OH,其表现出优异的抗肿瘤效果,治疗指数高。 还公开了含有至少一种有效量的上述化合物的抗肿瘤剂。