Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents

被引：72

作者：

Martins, Cristina

Gunaratnam, Mekala

Stuart, John

Makwana, Vaidahl

Greciano, Olga

Reszka, Anthony P.

Kelland, Lloyd R.

Neidle, Stephen

机构：

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

[2] St George Hosp, Sch Med, Antisoma Labs, London SW17 0QS, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 08期

关键词：

G-quadruplex; acridines; telomerase;

D O I：

10.1016/j.bmcl.2007.01.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design, synthesis, biophysical and biochemical evaluation is presented of a new series of benzylamino-substituted acridines as G-quadruplex binding telomerase inhibitors. Replacement of the previously reported anilino substituents by benzylamino groups results in enhanced quadruplex interaction, and for one compound, superior telomerase inhibitory activity. (c) 2007 Published by Elsevier Ltd.

引用

页码：2293 / 2298

页数：6

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