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당부분에서 4''-플루오린 또는 4''-아자이드로 치환된 3''-히드록시다우노루비신과 3''-히드록시독소루비신 유도체의 합성과 항암활성

Synthesis and Antitumor Activity of 3''-hydroxydaunorubicin and 3''-hydroxydoxorubicin Derivatives Substituted with 4''-fluorine or 4''-azide in Sugar Moiety

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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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