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Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3, 6-and 9-side chains on quadruplex binding, telomerase activity, and …

…, F Cuenca, M Gunaratnam, FA Tanious…

文献索引:Moore, Michael J. B.; Schultes, Christoph M.; Cuesta, Javier; Cuenca, Francisco; Gunaratnam, Mekala; Tanious, Farial A.; Wilson, W. David; Neidle, Stephen Journal of Medicinal Chemistry, 2006 , vol. 49, # 2 p. 582 - 599

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被引用次数: 167

摘要

The synthesis is reported of a group of 3, 6, 9-trisubstituted acridine compounds as telomeric quadruplex-stabilizing ligands with systematic variations at the 3-, 6-, and 9-positions. A new microwave-assisted methodology has been developed for trisubstituted acridine synthesis. Structure-activity relationships are reported using surface plasmon resonance and a fluorescence melting assay to examine quadruplex binding, together with a telomerase ...