Abstract
A series of novel 2,4,6-triarylpyridines have been synthesized and their interactions with intramolecular G-quadruplexes have been measured by Förster 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.
Original language | English |
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Pages (from-to) | 6154-6162 |
Number of pages | 9 |
Journal | Organic and Biomolecular Chemistry |
Volume | 9 |
Issue number | 17 |
DOIs | |
Publication status | Published - 7 Sept 2011 |
Externally published | Yes |