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[阿霉素及其类似物]

[Adriamycin and its analogs].

作者信息

Arcamone F

出版信息

Tumori. 1984 Apr 30;70(2):113-9. doi: 10.1177/030089168407000201.

Abstract

Among the biologically active metabolites produced by Streptomyces peucetius adriamycin (syn. doxorubicin) appeared the most effective anthracycline. Because of the low yield of the biosynthetic process, the chemical conversion of daunorubicin to adriamycin represent the key-step of the development of the drug. The therapeutic importance of adriamycin prompted us to begin since 1972 a research program aimed to the development of the second generation anthracyclines. The studies carried out during this research program allowed to discover three new synthetic anthracyclines, which, for the time being, are under clinical investigation: 4'- epidoxorubicin ( epirubicin ), 4-demethoxydaunorubicin ( idarubicin ) and 4'-deoxydoxorubicin ( esorubicin ). These compounds, like daunorubicin and doxorubicin, show affinity to DNA, but some of their pharmacological properties and metabolism in animals as well as in humans are different in respect to those of the parent drugs. Herein the stages of the search for new analogs and the outlooks of further progress in the filed of the antitumor anthracyclines are shortly reported.

摘要

在佩鲁贾链霉菌产生的生物活性代谢产物中,阿霉素(又名多柔比星)是最有效的蒽环类抗生素。由于生物合成过程产量低,柔红霉素化学转化为阿霉素是该药物研发的关键步骤。阿霉素的治疗重要性促使我们自1972年起开展一项旨在开发第二代蒽环类抗生素的研究计划。在该研究计划中进行的研究发现了三种新的合成蒽环类抗生素,目前它们正处于临床研究阶段:4'-表阿霉素(表柔比星)、4-去甲氧基柔红霉素(伊达比星)和4'-脱氧阿霉素(依索比星)。这些化合物与柔红霉素和阿霉素一样,对DNA具有亲和力,但它们在动物和人类中的一些药理特性及代谢与母体药物有所不同。本文简要报道了寻找新类似物的阶段以及抗肿瘤蒽环类药物领域进一步进展的前景。

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