title: Efficient Inhibition of Telomerase by Nickel-Salophen Complexes.
abstract: Four nickel(II)-salophen complexes containing alkyl-imidazolium chains connected at the ortho or meta positions were prepared: N,N'-bis(2-hydroxy-4-methyl-3H-imidazol-1-iumbenzylideneamino)phenylenediamine (1), N,N'-bis(2-hydroxy-3-methyl-3H-imidazol-1-iumbenzylideneamino)phenylenediamine (2), N,N'-bis(2-hydroxy-3-methyl-3H-imidazol-1-iumbenzylideneamino)methyl-3H-imidazol-1-iumphenylenediamine (3), and N,N'-bis(2-hydroxy-4-methyl-3H-imidazol-1-iumbenzylideneamino)methyl-3H-imidazol-1-iumphenylenediamine (4). They protect G-quadruplex DNA (G4 -DNA) against thermal denaturation and show KA values in the range of 7.4×10(5) to 4×10(7)  m(-1) for G4 -DNA models. Complex 4 exhibits an IC50 value of 70 nm for telomerase inhibition.
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France.
authors.forename: Laureline
authors.initials: L
authors.lastname: Lecarme
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France.
authors.forename: Enora
authors.initials: E
authors.lastname: Prado
authors.affiliation: ARNA laboratory, Inserm U1212, CNRS UMR 5320, Institut Européen de Chimie et Biologie IECB - Université de Bordeaux, 2 rue Robert Escarpit, 33607, Pessac, France.
authors.forename: Aurore
authors.identifier: 0000-0003-0868-3670
authors.initials: A
authors.lastname: De Rache
authors.affiliation: Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France.
authors.forename: Marie-Laure
authors.initials: ML
authors.lastname: Nicolau-Travers
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France.
authors.forename: Gisèle
authors.initials: G
authors.lastname: Gellon
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France.
authors.forename: Jérôme
authors.initials: J
authors.lastname: Dejeu
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France.
authors.forename: Thomas
authors.initials: T
authors.lastname: Lavergne
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France.
authors.forename: Hélène
authors.initials: H
authors.lastname: Jamet
authors.affiliation: Institut de Pharmacologie et de Biologie Structurale, 205 Route de Narbonne, 31077, Toulouse Cedex 4, France.
authors.forename: Dennis
authors.initials: D
authors.lastname: Gomez
authors.affiliation: ARNA laboratory, Inserm U1212, CNRS UMR 5320, Institut Européen de Chimie et Biologie IECB - Université de Bordeaux, 2 rue Robert Escarpit, 33607, Pessac, France.
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Mergny
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France.
authors.forename: Eric
authors.initials: E
authors.lastname: Defrancq
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France.
authors.forename: Olivier
authors.initials: O
authors.lastname: Jarjayes
authors.affiliation: Université Grenoble Alpes, Département de Chimie Moléculaire, UMR-5250, 38041, Grenoble Cedex 9, France. Fabrice.Thomas@ujf-grenoble.fr.
authors.forename: Fabrice
authors.initials: F
authors.lastname: Thomas
mesh_terms: D056831:Coordination Complexes / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D007700:Kinetics; D009532:Nickel / Q000737:chemistry*; D014176:Protein Biosynthesis / Q000187:drug effects; D012459:Salicylates / Q000737:chemistry*; D019098:Telomerase / Q000037:antagonists & inhibitors / Q000378:metabolism*; D042461:Vascular Endothelial Growth Factor A / Q000235:genetics / Q000378:metabolism
chemical_list: D056831:Coordination Complexes; D004791:Enzyme Inhibitors; D012459:Salicylates; D042461:Vascular Endothelial Growth Factor A; C090416:salophen; D009532:Nickel; D019098:Telomerase
keywords: DNA; G-quadruplexes; bioinorganic chemistry; nickel; salophen