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.
Laronze-Cochard
Marie
M
Université de Reims-Champagne-Ardenne, Institut de Chimie Moléculaire de Reims, CNRS UMR 6229, IFR 53 Biomolécules, Faculté de Pharmacie, 51 rue de Cognacq-Jay, F-51096 Reims, France.
Kim
Young-Min
YM
Brassart
Bertrand
B
Riou
Jean-François
JF
Laronze
Jean-Yves
JY
Sapi
Janos
J
D000166:Acridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes / Q000187:drug effects*; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D009691:Nucleic Acid Denaturation / Q000187:drug effects; D019098:Telomerase / Q000037:antagonists & inhibitors / Q000378:metabolism; D016615:Telomere / Q000187:drug effects*
D000166:Acridines; D000970:Antineoplastic Agents; D008024:Ligands; D019098:Telomerase