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包含二芳基脲支架和三唑连接体的G-四链体配体的点击化学组装。

Click chemistry assembly of G-quadruplex ligands incorporating a diarylurea scaffold and triazole linkers.

作者信息

Drewe William C, Neidle Stephen

机构信息

CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London, UK.

出版信息

Chem Commun (Camb). 2008 Nov 14(42):5295-7. doi: 10.1039/b814576h. Epub 2008 Sep 30.

Abstract

A series of diarylurea ligands were designed to interact selectively with G-quadruplexes and were synthesised using copper(I) catalysed 'click' chemistry to incorporate the 1,4-substituted 1,2,3-triazole ring into the core of the ligands; the optimal ligands demonstrate a high degree of selective telomeric G-quadruplex stabilisation and are not cytotoxic in several cancer cell lines.

摘要

设计了一系列二芳基脲配体,使其与G-四链体选择性相互作用,并利用铜(I)催化的“点击”化学将1,4-取代的1,2,3-三唑环引入配体核心进行合成;最佳配体表现出高度的端粒G-四链体选择性稳定作用,并且在几种癌细胞系中无细胞毒性。

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