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    • 7. 发明授权
    • Ecteinascidin analogs for use as antitumour agents
    • 用作抗肿瘤剂的抗坏血酸类抗生素
    • US07763615B2
    • 2010-07-27
    • US10485536
    • 2002-08-06
    • Pilar GallegoCarmen CuevasSimon MuntIgnacio ManzanaresValentin Martinez
    • Pilar GallegoCarmen CuevasSimon MuntIgnacio ManzanaresValentin Martinez
    • A01N43/58A01N43/60A61K31/50A61K31/495C07D487/00C07D491/00C07D513/00
    • C07D515/22
    • Derivatives of ecteinascidin 736 of general formula (I) wherein the groups R1, R2, R3, R4 and R5 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, C(═O)R′, C(═O)OR′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclic; wherein X is independently selected of OR′, CN, (═O), or H; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein m is 0, 1 or 2; and wherein n is 0, 1, 2, 3, or 4, and their use as antitumoral agent.
    • 基团R 1,R 2,R 3,R 4和R 5各自独立地选自H,OH,OR',SH,SR',SOR',SO 2 R',C的通式(I)的抗坏血酸素736衍生物 (= O)R',C(= O)OR',NO 2,NH 2,NHR',N(R')2,NHC(O)R',CN,卤素,= O,取代或未取代的C 1 -C 25烷基 取代或未取代的C 2 -C 18烯基,取代或未取代的C 2 -C 18炔基,取代或未取代的芳基,取代或未取代的杂环基; 其中X独立地选自OR',CN,(= O)或H; 其中每个R'基团独立地选自H,OH,NO 2,NH 2,SH,CN,卤素,= O,C(= O)H,C(= O)CH 3,CO 2 H, 未取代的C 1 -C 25烷基,取代或未取代的C 2 -C 18烯基,取代或未取代的C 2 -C 18炔基,取代或未取代的芳基; 其中m为0,1或2; 并且其中n为0,1,2,3或4,并且其用作抗肿瘤剂。