Acridine conjugates of 3-Clip-Phen:: Influence of the linker on the synthesis and the DNA cleavage activity of their copper complexes

被引：22

作者：

Boldron, C ^{[1
]}

Ross, SA ^{[1
]}

Pitié, M ^{[1
]}

Meunier, B ^{[1
]}

机构：

[1] CNRS, Chim Coordinat Lab, F-31077 Toulouse 4, France

来源：

BIOCONJUGATE CHEMISTRY | 2002年 / 13卷 / 05期

关键词：

D O I：

10.1021/bc020013x

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

To increase the DNA cleavage activity and the cell delivery of the bis(phenanthroline) DNA cleaver "3-Clip-Phen", conjugates between 3-Clip-Phen and the intercalators acridine and 6-chloro-2-methoxyacridine, through amino acid linkers of various length, were prepared. After complexation with CuCl2, the ability of these conjugates to cleave PhiX 174 DNA in the presence of a reductant and air was compared. The results indicated that (i) the coupling of 3-Clip-Phen to an acridine derivative increased the DNA cleavage efficiency of the copper complexes, (ii) the acridine derivatives were more active than 6-chloro-2-methoxyacridine derivatives, (iii) the linker length influenced cleavage efficiency, the highest DNA cleavage activity being obtained for an aminocaproic spacer.

引用

页码：1013 / 1020

页数：8

共 35 条

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