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1: J Am Chem Soc. 2006 Dec 20;128(50):15972-3.
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Stabilization of G-quadruplex DNA by highly selective ligands via click chemistry.

Moorhouse AD, Santos AM, Gunaratnam M, Moore M, Neidle S, Moses JE.

Department of Pharmaceutical and Biological Chemistry, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.

A series of G-quadruplex stabilizing compounds have been prepared via click chemistry employing the Cu(I)-catalyzed Huisgen reaction. These compounds were shown to bind tightly to G-quadruplex DNA even in the presence of competing high concentrations of duplex DNA. Furthermore, a modified TRAP assay has shown that some of these compounds also inhibit telomerase at low micromolar concentration.

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PMID: 17165715 [PubMed - indexed for MEDLINE]