Premium
Efficient Inhibition of Telomerase by Nickel–Salophen Complexes
Author(s) -
Lecarme Laureline,
Prado Enora,
De Rache Aurore,
NicolauTravers MarieLaure,
Gellon Gisèle,
Dejeu Jérôme,
Lavergne Thomas,
Jamet Hélène,
Gomez Dennis,
Mergny JeanLouis,
Defrancq Eric,
Jarjayes Olivier,
Thomas Fabrice
Publication year - 2016
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201600171
Subject(s) - nickel , chemistry , dna , stereochemistry , alkyl , telomerase , medicinal chemistry , biochemistry , organic chemistry , gene
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‐3 H ‐imidazol‐1‐iumbenzylideneamino)phenylenediamine ( 1 ), N , N ′‐bis(2‐hydroxy‐3‐methyl‐3 H ‐imidazol‐1‐iumbenzylideneamino)phenylenediamine ( 2 ), N , N ′‐bis(2‐hydroxy‐3‐methyl‐3 H ‐imidazol‐1‐iumbenzylideneamino)methyl‐3 H ‐imidazol‐1‐iumphenylenediamine ( 3 ), and N , N ′‐bis(2‐hydroxy‐4‐methyl‐3 H ‐imidazol‐1‐iumbenzylideneamino)methyl‐3 H ‐imidazol‐1‐iumphenylenediamine ( 4 ). They protect G‐quadruplex DNA (G 4 ‐DNA) against thermal denaturation and show K A values in the range of 7.4×10 5 to 4×10 7 m −1 for G 4 ‐DNA models. Complex 4 exhibits an IC 50 value of 70 n m for telomerase inhibition.