期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 9, 期 17, 页码 6154-6162出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c1ob05560g
关键词
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资金
- Australian Research Council (ARC)
- University of Western Australia
- INCa
- Region Aquitaine
- Fondation pour la Recherche Medicale
- ANR
- Ligue contre le Cancer
- comite de Gironde
- IFR66
A series of novel 2,4,6-triarylpyridines have been synthesized and their interactions with intramolecular G-quadruplexes have been measured by Forster Resonance Energy Transfer (FRET) melting and Fluorescent Intercalator Displacement (FID) assays. A few of these compounds exhibit stabilization of G4-DNA that is comparable to other benchmark G4-DNA ligands with fair to excellent G4-DNA vs. duplex selectivity and significant cytotoxicity towards HeLa cells. The nature of the 4-aryl substituents along with side chain length governs the G4-DNA stabilization ability of the compounds. In addition, we demonstrate that there is a strong correlation between the ability of the compounds to stabilize the same G4-DNA sequence in K+ and Na+ conditions and a strong correlation between the ability of the compounds to stabilize different G4-DNA sequences in K+ or Na+ buffer.
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