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BENZ(5,6)ISOINDOLO(2,1-B)ISOQUINOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
BENZ(5,6)ISOINDOLO(2,1-B)ISOQUINOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
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机译:苯并(5,6)异吲哚(2,1-B)异喹啉衍生物和药物成分
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摘要
There are provided compounds of general formula (1) CHEM (wherein R1 is a hydrogen atom or a methyl group; R2 is a hydrogen or halogen atom or a methyl group; and one of R3 and R4 is a hydrogen atom and the other is a group -NR5R6 [where R5 is a hydrogen atom and R6 is a group -COCH2NR7R8 (wherein R7 and R8, which may be the same or different, each represents a hydrogen atom or a C3-7 cycloalkyl group or a C1-4 alkyl group optionally substituted by a hydroxyl or benzoyloxy group, or -NR7R8 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring an oxygen or sulphur atom or a group -NH-or -N(R)- where R is a C1-4 alkyl group optionally substituted by a hydroxyl group) or R6 is a group -COCH2NH(CH2)nNR7R8 (where n is an integer from 2 to 5 inclusive and R7, R8 and -NR7R8 are as defined above) or R6 is a group -N=CR9R10 (where R9 is a hydrogen atom or a C1-4 alkyl group and R10 is a C1-4 alkyl group optionally substituted by a group -NR7R8 and R7, R8 and -NR7R8 are as defined above) or R5 is a hydrogen atom or an acyl group and R6 is a group -(CH2)nNR7R8 (where n, R7, R8 and -NR7R8 are as defined above)]) and salts thereof. The compounds exhibit anti-cancer activity.
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机译:提供了通式(1)的化合物(其中R 1是氢原子或甲基; R 2是氢或卤素原子或甲基;和R 3之一) R 4为氢原子,另一个为-NR 5 R 6基团[其中R 5为氢原子,R 6为-COCH 2 NR 7 R 8基团>(其中R 7和R 8可以相同或不同,各自代表氢原子或C 3-7环烷基或任选被羟基或苯甲酰氧基取代的C 1-4烷基,或-NR 7 R 8形成具有5-7个环成员的饱和杂环氨基,并且在环中任选地包含氧或硫原子或-NH-或-N(R)-基团,其中R为任选地被羟基取代的C 1-4烷基)或R 6是基团-COCH 2 NH(CH 2)n NR 7 R 8(其中n是2至5之间的整数,R 7是, R 8和-NR 7 R 8如上定义)或R 6为基团-N = CR 9 R 1 0(其中R 9为氢)原子或碳数1〜4的烷基和R 1 <0> i任选地被-NR 7 R 8和R 7,R 8和-NR 7 R 8的基团取代的C 1-4烷基如上所定义)或R 5 R 6是氢原子或酰基,R 6是基团-(CH 2)n NR 7 R 8(其中,n,R 7,R 8和-NR 7 R 8 >如上所定义)])及其盐。该化合物具有抗癌活性。
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