Synthesis and biological evaluation of novel 4,5-bis(dialkylaminoalkyl)-substituted acridines as potent telomeric G-quadruplex ligands

Several 4,5-bis(dialkylaminoalkyl)-substituted acridines have been prepared starting from acridine and their telomeric G-quadruplex stabilizing properties were evaluated using FRET melting and TRAP (Telomerase Repeat Amplification Protocol Assay) experiments. Some 4,5-bis(dialkylaminoalkyl)-substitu...

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Veröffentlicht in:	European journal of medicinal chemistry 2009-10, Vol.44 (10), p.3880-3888
Hauptverfasser:	Laronze-Cochard, Marie, Kim, Young-Min, Brassart, Bertrand, Riou, Jean-François, Laronze, Jean-Yves, Sapi, Janos
Format:	Artikel
Sprache:	eng
Schlagworte:	4,5-Disubstituted acridine Acridines - chemical synthesis Acridines - chemistry Acridines - pharmacology Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Cell Line, Tumor Fluorescence Resonance Energy Transfer G-quadruplex ligand G-Quadruplexes - drug effects General aspects Humans Ligands Medical sciences Molecular Structure Nucleic Acid Denaturation - drug effects Pharmacology. Drug treatments Telomerase - antagonists & inhibitors Telomerase - metabolism Telomere Telomere - drug effects
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Zusammenfassung:	Several 4,5-bis(dialkylaminoalkyl)-substituted acridines have been prepared starting from acridine and their telomeric G-quadruplex stabilizing properties were evaluated using FRET melting and TRAP (Telomerase Repeat Amplification Protocol Assay) experiments. Some 4,5-bis(dialkylaminoalkyl)-substituted acridines have been prepared and their telomeric G-quadruplex stabilizing properties were evaluated. [Display omitted]
ISSN:	0223-5234 1768-3254
DOI:	10.1016/j.ejmech.2009.04.021