| 摘要 |
A new composition contains ascidemin derivatives (I) and (II) as cytotoxic agents. A new composition contains ascidemin derivatives (I) and (II) or their acid addition salts as cytotoxic agents. X = O, =NH, or =N-OH; R1 = H, halo, NO2, -NR8R9; R8, R9 = H or 1-4C alkyl; R2 = H or halo; R3 = H, halo, 1-4C alkyl, 1-6C alkoxy, guanidino, -NR10R11 or -(CH2)n-Y; R10, R11 = H, 1-4C alkyl, or phenyl 1-4C alkyl; Y = CN, -CH(O-Et)2, 1-6C alkoxy, -O-(CH2)2-N-(CH3)2, or -N(CH3)2; n = 1-3; R4 = H, halo, NO2, -NR12R13; R12 and R13 = H or 1-4C alkyl; R5 - R7 = H, halo, 1-6C alkyl or alkoxy, OH, 1-6C alkoxy 1-6C alkyl, 1-4C alkyl carbonyl 1-4C alkyl, CHO, COOH, CN, -COOR14, -CONR14R15, -NHCOR14 or -NR14R15, -phenyl-COCH3, -phenyl-COCH=CH-N(CH3)2, morpholino, NO2, -SO3H, -CH2-N(CH2-COOR17)-COOR16 or -CH2-N(CH2-Ar)-COOR16; R14, R15 = H, 1-6C alkyl, -phenyl-COCH3, or -CH2-CH2-N(CH3)2; R16, R17 = 1-6C alkyl; Ar = 6-14C aryl; except for those compounds of formula (I) in which X = O and R1 - R7 = H or R1 and R3 - R7 = H, R2 = Br, and the compound of formula (Ia) in which X = O and R1 - R7 = H. Independent claims are also included for: (1) new compounds of formulae (I) and (II) or their acid addition salts, with the additional exclusion of compounds of formula (I) in which X = O and R1, R2, R4 - R7 = H and R3 = OCH3, or in which X = O and R1 - R3, R4 - R7 = H and R5 = OH or OCH3, or in which X = O and R1 = NO2 and R2 - R7 = H; and (2) the preparation of (Ia).
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