Stabilization of G-quadruplex DNA by highly selective ligands via click chemistry

被引:222
作者
Moorhouse, Adam D.
Santos, Ana Mafalda
Gunaratnam, Mekala
Moore, Michael
Neidle, Stephen
Moses, John E.
机构
[1] Univ London, Sch Pharm, CRUK Biomol Struct Grp, London WC1N 1AX, England
[2] Univ London, Dept Pharmaceut & Biol Chem, London WC1N 1AX, England
关键词
D O I
10.1021/ja0661919
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of G-quadruplex stabilizing compounds have been prepared via click chemistry employing the Cu(I)-catalyzed Huisgen reaction. These compounds were shown to bind tightly to G-quadruplex DNA even in the presence of competing high concentrations of duplex DNA. Furthermore, a modified TRAP assay has shown that some of these compounds also inhibit telomerase at low micromolar concentration. Copyright © 2006 American Chemical Society.
引用
收藏
页码:15972 / 15973
页数:2
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