Looking for Efficient G-Quadruplex Ligands: Evidence for Selective Stabilizing Properties and Telomere Damage by Drug-Like Molecules

被引：47

作者：

Pagano, Bruno ^{[1
]}

Amato, Jussara ^{[1
]}

Iaccarino, Nunzia ^{[1
]}

Cingolani, Chiara ^{[2
]}

Zizza, Pasquale ^{[2
]}

Biroccio, Annamaria ^{[2
]}

Novellino, Ettore ^{[1
]}

Randazzo, Antonio ^{[1
]}

机构：

[1] Univ Naples Federico II, Dept Pharm, I-80131 Naples, Italy

[2] Regina Elena Inst Canc Res, Expt Chemotherapy Lab, I-00158 Rome, Italy

来源：

CHEMMEDCHEM | 2015年 / 10卷 / 04期

关键词：

anticancer agents; biological activity; DNA recognition; DNA structures; G-quadruplexes; DNA; BINDING; DESIGN; SUPPRESSION; COMPLEXES; DISCOVERY; FORMS;

D O I：

10.1002/cmdc.201402552

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

There is currently significant interest in the development of G-quadruplex-interactive compounds, given the relationship between the ability to stabilize these non-canonical DNA structures and anticancer activity. In this study, a set of biophysical assays was applied to evaluate the binding of six drug-like ligands to DNA G-quadruplexes with different folding topologies. Interestingly, two of the investigated ligands showed selective G-quadruplex-stabilizing properties and biological activity. These compounds may represent useful leads for the development of more potent and selective ligands.

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收藏

页码：640 / 649

页数：10

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