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在柔红霉素和亚德里亚霉素类似物的研究中,为改进抗肿瘤活性,降低心脏毒性,曾合成了一系列柔红酮和亚德里亚霉酮的脂环氨基酸酯类化合物。其中7-O-(反式-4′-氨基环己烷甲酰)亚德里亚霉酮(Ⅰ)(图1)在小鼠白血病L7712或P388抑瘤试验中给出了与亚德里亚霉素相当的生命延长率。
In studies of daunorubicin and adriamycin analogues, a series of cycloaliphatic aminoester esters of daunorubicin and adriamycin have been synthesized to improve antitumor activity and reduce cardiotoxicity. Among them, 7-O- (trans-4’-aminocyclohexanecarboxamido) adriamycinone (I) (FIG. 1) was given in the mouse leukemia L7712 or P388 tumor- Sufficient life extension rate.