Efficient Inhibition of Telomerase by Nickel–Salophen Complexes

Laureline Lecarme; Enora Prado; Aurore De Rache; Marie Laure Nicolau-Travers; Gisèle Gellon; Jérôme Dejeu; Thomas Lavergne; Hélène Jamet; Dennis Gomez; Jean Louis Mergny; Eric Defrancq; Olivier Jarjayes; Fabrice Thomas

doi:10.1002/cmdc.201600171

Efficient Inhibition of Telomerase by Nickel–Salophen Complexes

Laureline Lecarme
, Enora Prado
, Aurore De Rache
, Marie Laure Nicolau-Travers
, Gisèle Gellon
, Jérôme Dejeu
, Thomas Lavergne
, Hélène Jamet
, Dennis Gomez
, Jean Louis Mergny
, Eric Defrancq
, Olivier Jarjayes
, Fabrice Thomas

LTHE (UMR 5564 CNRS/IRD/Université de Grenoble)
INSERM, U869, IECB
Institut de Pharmacologie et de Biologie Structurale

Research output: Contribution to journal › Article › peer-review

23 Citations (Scopus)

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 K_Avalues in the range of 7.4×10⁵to 4×10⁷m⁻¹for G₄-DNA models. Complex 4 exhibits an IC₅₀value of 70 nm for telomerase inhibition.

Original language	English
Pages (from-to)	1133-1136
Number of pages	4
Journal	ChemMedChem
DOIs	https://doi.org/10.1002/cmdc.201600171
Publication status	Published - 1 Jan 2016
Externally published	Yes

Keywords

DNA
G-quadruplexes
bioinorganic chemistry
nickel
salophen

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10.1002/cmdc.201600171

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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 KAvalues in the range of 7.4×105to 4×107m−1for G4-DNA models. Complex 4 exhibits an IC50value of 70 nm for telomerase inhibition.",

keywords = "DNA, G-quadruplexes, bioinorganic chemistry, nickel, salophen",

author = "Laureline Lecarme and Enora Prado and \{De Rache\}, Aurore and Nicolau-Travers, \{Marie Laure\} and Gis{\`e}le Gellon and J{\'e}r{\^o}me Dejeu and Thomas Lavergne and H{\'e}l{\`e}ne Jamet and Dennis Gomez and Mergny, \{Jean Louis\} and Eric Defrancq and Olivier Jarjayes and Fabrice Thomas",

note = "Publisher Copyright: {\textcopyright} 2016 WILEY-VCH Verlag GmbH \& Co. KGaA, Weinheim",

year = "2016",

month = jan,

day = "1",

doi = "10.1002/cmdc.201600171",

language = "English",

pages = "1133--1136",

journal = "ChemMedChem",

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TY - JOUR

T1 - Efficient Inhibition of Telomerase by Nickel–Salophen Complexes

AU - Lecarme, Laureline

AU - Prado, Enora

AU - De Rache, Aurore

AU - Nicolau-Travers, Marie Laure

AU - Gellon, Gisèle

AU - Dejeu, Jérôme

AU - Lavergne, Thomas

AU - Jamet, Hélène

AU - Gomez, Dennis

AU - Mergny, Jean Louis

AU - Defrancq, Eric

AU - Jarjayes, Olivier

AU - Thomas, Fabrice

PY - 2016/1/1

Y1 - 2016/1/1

N2 - 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 KAvalues in the range of 7.4×105to 4×107m−1for G4-DNA models. Complex 4 exhibits an IC50value of 70 nm for telomerase inhibition.

AB - 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 KAvalues in the range of 7.4×105to 4×107m−1for G4-DNA models. Complex 4 exhibits an IC50value of 70 nm for telomerase inhibition.

KW - DNA

KW - G-quadruplexes

KW - bioinorganic chemistry

KW - nickel

KW - salophen

U2 - 10.1002/cmdc.201600171

DO - 10.1002/cmdc.201600171

M3 - Article

C2 - 27166712

AN - SCOPUS:84973652535

SN - 1860-7179

SP - 1133

EP - 1136

JO - ChemMedChem

JF - ChemMedChem

ER -

Efficient Inhibition of Telomerase by Nickel–Salophen Complexes

Abstract

Keywords

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