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KMID : 0370219960400020117
Yakhak Hoeji
1996 Volume.40 No. 2 p.117 ~ p.125
Synthesis and Antitumor Activity of 3¡¯¡¯-hydroxydaunorubicin and 3¡¯¡¯-hydroxydoxorubicin Derivatives Substituted with 4¡¯¡¯-fluorine or 4¡¯¡¯-azide in Sugar Moiety
¿Á±¤´ë/Ok KD
¹ÚÁ¤¹è/±è¹®¼º/Á¤µ¿À±/¾çÁßÀÍ/Park JB/Kim MS/Jung DY/Yang JI
Abstract
3¡¯¡¯-Deamino-3¡¯¡¯-hydroxy-4¡¯¡¯-fluoro- or 3¡¯¡¯-deamino-3¡¯¡¯-hydroxy-4¡¯¡¯-azido-daunorubicin(6,8) and -doxorubicin(7,9) have been synthesized, respectively. Compounds 7,8 and 9 were more cytotoxic than daunorubicin(1) and doxorubicin(2) against L1210 murine leukemic cell in vitro. When administered intraperitoneally for 9 days starting 1 day after tumor inoculation, compounds 7(T/C 605%) and 9(T/C 488%) showed significant antitumor activity for ip-inoculuated L1210 murine leukemia at wide range of doses.
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