Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands

被引：119

作者：

Cuenca, Francisco ^{[1
]}

Greciano, Olga ^{[1
]}

Gunaratnam, Mekala ^{[1
]}

Haider, Shozeb ^{[1
]}

Munnur, Deeksha ^{[1
]}

Nanjunda, Rupesh ^{[2
]}

Wilson, W. David ^{[2
]}

Neidle, Stephen ^{[1
]}

机构：

[1] Univ London, Sch Pharm, CRUK Biomol Struct Grp, London WC1N 1AX, England

[2] Georgia State Univ, Dept Chem, Atlanta, GA 30303 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 05期

关键词：

G-quadruplex; telomere; telomerase inhibition;

D O I：

10.1016/j.bmcl.2008.01.050

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of tri- and tetra-substituted naphthalene diimides have been designed and synthesized. Several compounds show exceptional affinity for telomeric G-quadruplex DNA in classical and competition FRET assays and SPR studies. They inhibit telomerase in the TRAP assay, and show potent senescence-based short-term anti-proliferative effects on MCF7 and A549 cancer cell lines, and localize in the nucleus and particularly the nucleolus of MCF7 cells. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：1668 / 1673

页数：6