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KMID : 0370219960400010010
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Yakhak Hoeji
1996 Volume.40 No. 1 p.10 ~ p.18
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Synthesis and Antitumor Activity of 7-O-(alpha-L-rhamnopyranosyl) or 7-O-(4’’-amino-alpha-L-rhamnopyranosyl)-daunomycinone and -adriamycinone Derivatives
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옥광대/Ok KD
박정배/김문성/정동윤/안상용/배중석/양중익/Park JB/Kim MS/Jung DY/An SY/Bae CS/Yang JI
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Abstract
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Daunirubicin and doxorubicin analogues (5,7,8,9,) in which the natural amino sugar, daunosamine, is replaced by rhamnopyranosyl or 4’’-amino rhamnopyranosyl residues have been prepared. The in vitro cytotoxicity of compound 5 or 7 was similar to that of doxorubicin for P388 murine leukemic cell line. But compound 8 or 9 was less cytotoxic than doxorubicin. When administered intravenously on day 1, compound 9 showed antitumor activity comparable to that of doxorubicin against ip-inoculated L1210 murine leukemia and found to be less toxic than doxorubicin. But the in vivo antitumor activity of compound 7 or 8 was inferior to that of doxorubicin.
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