New highly hydrosoluble and not self-aggregated perylene derivatives with three and four polar side-chains as G-quadruplex telomere targeting agents and telomerase inhibitors

被引：40

作者：

Franceschin, Marco

Pascucci, Emanuela

Alvino, Antonello

D'Ambrosio, Danilo

Bianco, Armandodoriano

Ortaggi, Giancarlo

Savino, Maria

机构：

[1] Univ Roma La Sapienza, Dipartimento Chim, I-00185 Rome, Italy

[2] Univ Roma La Sapienza, Dipartimento Genet & Biol Mol, I-00185 Rome, Italy

[3] Univ Roma La Sapienza, CNR, Ist Chim Biomol, I-00185 Rome, Italy

[4] Univ Roma La Sapienza, CNR, Ist Biol & Patol Mol, I-00185 Rome, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 09期

关键词：

hydrosoluble perylene derivatives; G-quadruplex; telomerase inhibitors;

D O I：

10.1016/j.bmcl.2007.02.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Four new perylene derivatives with three and four basic side-chains are reported here as G-cluadruplex interactive compounds. The new perylene derivatives are readily soluble in water and not self-aggregated, in contrast to what happens with the previously reported two side-chain perylene derivatives. All four compounds are able to induce the G-cluadruplex and to inhibit 50% of telomerase activity at about 5 mu M concentration, showing a similar efficiency with respect to each other. Molecular modelling studies are presented to try to explain these findings. (C) 2007 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2515 / 2522

页数：8

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