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1、机制NClClHClNClClONClClHOONClClHOOHNH2NClClHOOHNHONHPOONClCl1 2 H2ONPOONHClClNHPOONHClOPNNNSPNNNClNHNClONO3 2 1ClNNHONOClNNHONO OHOHOOHOHHNNOH3CNOOHOHOOHOHHNNONOClH3CSOOOOSCH3OOSOOSOOOOSOOOR-HN+RNH2OSOO+H+SOOSOOOOR-HN+BrBrOHHHOHHOHHOHBrBrOHHHOHHOHOHHOOHORHHOR PtClH3NClH3NPtOH3NOH3NOOH2NNH2PtOOOO PtClH
2、3NClH3N双齿配位体代替单齿可增加活性取代体有适当的水解速率烷基伯胺或环烷基伯胺取代可明显增加治疗指数中性配合物比离子配合物活性高整体平面正方形和八面体构型活性高尿嘧啶衍生物胞嘧啶衍生物HNNHOFOClOCH3OFOCH3OFOCH3OHOKFAcNH2HCOOC2H5CH3ONaOCH3ONaOFCH3OHCH3ONaHClH2OHNNHOFONNOHFOH3CH3CONH2NHNNH2NOHHHOHOHHOOHHClNNNHNOHNNNHNSHH2ONNNNSNaSO3Na2H2ONNNHNSHI2NNNHNSNNNHNSNa2SO3H2ONNNNSNaSO3Na2H2O +NNNH
3、NSHNNNHNSHH2NNNNNH2NOHNHNHOOOHHOOHNNNNH2NNH2NNHOOOHHOOHCH3ONCH3CH3NH2OOL-ThrL-ThrOD-ValOD-ValOL-MevalL- MevalSarL-ProPro-LSarNNHNH2NONH2ONH2HHCH3H2NOHNNHO H3CHOH3CHNONHOSNHHHHHHOHCH3NSROONNHOOHOHHOOOOHONH2OOHHBleomycin A2 R=Bleomycin B2 R=Bleomycin A5 R=Bleomycin R=HNS+X-CH3HNNHNH2NHHNHNNH2HNHNCH3OO
4、OH3COHOHOR1OHOH3CNH2R3R2OHDoxorubicin （多柔比星） R1=R3=-OH R2=-HDaunorubicin (柔红霉素) R1=R2=-H R3=-OHEpitubicin （表柔比星） R1=R2=-OH R3=-HOOHOHNHNHOHNOHNHOHNNOOOOHH3CHOHNNOHCH3OOH3COH3CNNR1OHOHHOR2CH3R3 R1 R2 R3长春碱 (Vinblastine) -CH3 -OCH3 -COCH3长春新碱 (Vincristine) -CHO -OCH3 -COCH3长春地辛（Vindesin） -CH3 -NH2 -HR1NHOOOH3COHH3COCH3OHCH3R2OOOHOOAcHOCH3OOCH3CH3CH3-H32131219111 2345678910141517161820 R1 R2紫杉醇 Taxol紫杉特尔 Taxotere