Drewe William C, Neidle Stephen
CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London, UK.
Chem Commun (Camb). 2008 Nov 14(42):5295-7. doi: 10.1039/b814576h. Epub 2008 Sep 30.
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.
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。
