Design of site specific DNA damaging agents for generation of multiply damaged sites

被引:20
作者
Martelli, A [1 ]
Constant, JF [1 ]
Demeunynck, M [1 ]
Lhomme, J [1 ]
Dumy, P [1 ]
机构
[1] Univ Grenoble 1, CNRS, LEDSS, F-38041 Grenoble 9, France
关键词
DNA damaging agents; acridines; abasic site;
D O I
10.1016/S0040-4020(02)00345-9
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We describe the synthesis and DNA damaging activities of hybrid molecules in which a purine (adenine) is linked to an intercalating chromophore (acridine) by a polyamino linker. A DNA damaging agent, phenanthroline or para-nitrobenzamide, is tethered to the acridine moiety at various positions. Our goal is to induce upon activation other lesions in close proximity to the abasic site and therefore create cytotoxic multiply damaged sites. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:4291 / 4298
页数:8
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