Efficient Inhibition of Telomerase by Nickel-Salophen Complexes

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• 作者：Dr. Laureline Lecarme ; Dr. Enora Prado ; Dr. Aurore De Rache ; Marie-Laure Nicolau-Travers ; Gisè ; le Gellon ; Dr. Jé ; rô ; me Dejeu ; Dr. Thomas Lavergne ; Dr. Hé ; lè ; ne Jamet ; Dr. Dennis Gomez ; Jean-Louis Mergny ; Prof. Eric Defrancq ; Dr. Olivier Jarjayes and Prof. Fabrice Thomas
• 刊名：ChemMedChem
• 出版年：2016
• 出版时间：June 6, 2016
• 年：2016
• 卷：11
• 期：11
• 页码：1133-1136
• 全文大小：626K
• ISSN：1860-7187

文摘

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 K_A values in the range of 7.4×10⁵ to 4×10⁷ m⁻¹ for G₄-DNA models. Complex 4 exhibits an IC₅₀ value of 70 nm for telomerase inhibition.