Efficient Inhibition of Telomerase by Nickel–Salophen Complexes
Copyright policy )Efficient Inhibition of Telomerase by Nickel–Salophen Complexes
AbstractFour 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 7.4×105 to 4×107 m−1 for G4‐DNA models. Complex 4 exhibits an IC50 value of 70 nm for telomerase inhibition.
- University of Grenoble France
- University of Bordeaux France
- Institut Européen de Chimie et Biologie France
- University of Bordeaux France
- Grenoble Alpes University France
Vascular Endothelial Growth Factor A, Molecular Biology/Biochemistry [q-bio.BM], [CHIM.THER]Chemical Sciences/Medicinal Chemistry, Salicylates, [CHIM.THEO]Chemical Sciences/Theoretical and/or physical chemistry, G-Quadruplexes, Kinetics, [SDV.BBM.BC]Life Sciences [q-bio]/Biochemistry, [CHIM.ANAL]Chemical Sciences/Analytical chemistry, Coordination Complexes, Nickel, Protein Biosynthesis, Fluorescence Resonance Energy Transfer, Humans, [CHIM.COOR]Chemical Sciences/Coordination chemistry, Enzyme Inhibitors, Telomerase, HeLa Cells
Vascular Endothelial Growth Factor A, Molecular Biology/Biochemistry [q-bio.BM], [CHIM.THER]Chemical Sciences/Medicinal Chemistry, Salicylates, [CHIM.THEO]Chemical Sciences/Theoretical and/or physical chemistry, G-Quadruplexes, Kinetics, [SDV.BBM.BC]Life Sciences [q-bio]/Biochemistry, [CHIM.ANAL]Chemical Sciences/Analytical chemistry, Coordination Complexes, Nickel, Protein Biosynthesis, Fluorescence Resonance Energy Transfer, Humans, [CHIM.COOR]Chemical Sciences/Coordination chemistry, Enzyme Inhibitors, Telomerase, HeLa Cells
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