Novel anthracycline oligosaccharides: Influence of chemical modifications of the carbohydrate moiety on biological activity

被引:34
作者
Cipollone, A
Berettoni, M
Bigioni, M
Binaschi, M
Cermele, C
Monteagudo, E
Olivieri, L
Palomba, D
Animati, F
Goso, C
Maggi, CA
机构
[1] Menarini Ric, I-00040 Monte Porzio Catone, Italy
[2] Menarini Ric, I-50131 Florence, Italy
关键词
D O I
10.1016/S0968-0896(01)00411-4
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Several observations highlight the importance of the carbohydrate moiety for the biological activity of antitumoural anthracyclines. Here is reported the synthesis, cytotoxicity and topoisomerase II-mediated DNA cleavage intensity of the new oligosaccharide anthracyclines 1-4 modified in the sugar residue. Evaluation of cytotoxic potency on different cell lines, resulted in quite similar values among the different analogues. On the other hand, topoisomerase II-mediated DNA breaks level was different for the various compounds. and was not related to cytotoxicity, thus supporting previous observations reported for some monosaccharide anthracyclines modified in the carbohydrate portion. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1459 / 1470
页数:12
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