Pharmacological profile of new deamino analogues of sabarubicin (MEN 10755)

被引：3

作者：

Bigioni, M ^{[1
]}

Salvatore, C ^{[1
]}

Cipollone, A ^{[1
]}

Berettoni, M ^{[1
]}

Maggi, CA ^{[1
]}

Binaschi, M ^{[1
]}

机构：

[1] Menarini Ric SpA, Dept Pharmacol, I-00040 Monte Porzio Catone, Italy

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2005年 / 2卷 / 01期

关键词：

sabarubicin; MEN; 10755; 10959; 12297; anthracycline disaccharides; DNA topoisomerase;

D O I：

10.2174/1570180053398307

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Sabarubicin (MEN 10755) is the progenitor of a third generation of synthetic anthracycline oligosaccharides. Sabarubicin deamino analogues MEN 10959 and MEN 12297 were evaluated for topoisomerase II poisoning, cytotoxic potency and antitumor activity in human xenografts. The new analogues were able to induce DNA cleavage mediated by both DNA topoisomerase II alpha and beta and a good correlation was found regarding their cytotoxic activity. The two analogues possess also a different spectrum of antitumor activity, compared to sabarubicin.

引用

页码：68 / 73

页数：6

共 25 条

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