Selective Recognition of G-Quadruplex by Structural Tuning of Heteroaromatic Scaffolds and Side Chains.

In this study, carbazole () and dibenzofuran () derivatives were synthesized to examine their effect on the biomolecular recognition of G-quadruplex (G4) targets. Biophysical studies revealed that , a carbazole derivative, exhibits a specific affinity and effectively stabilizes the G4. Molecular modeling suggests a stable interaction of with the terminal G-tetrad of G4.

Triazolyl Dibenzo[]phenazines Stabilize Telomeric G-quadruplex and Inhibit Telomerase.

We herein report the synthesis and biophysical evaluation of triazolyl dibenzo[]phenazine derivatives as a novel class of G-quadruplex ligands. The aromatic core facilitates π-π interaction and the flexible, protonatable side chains interact with the phosphate backbone of DNA electrostatic interactions. Förster resonance energy transfer (FRET) melting assay and isothermal titration calorimetry (ITC) studies suggest that these ligands show binding preference for the G-quadruplex over G-quadruplexes found in the promoter region of various oncogenes and duplex DNA.

Chemical Regulation of DNA i-Motifs for Nanobiotechnology and Therapeutics.

DNA sequences rich in cytosine have the propensity, under acidic pH, to fold into four-stranded intercalated DNA structures called i-motifs. Recent studies have provided significant breakthroughs that demonstrate how chemists can manipulate these structures for nanobiotechnology and therapeutics. The first section of this Minireview discusses the development of advanced functional nanostructures by synthetic conjugation of i-motifs with organic scaffolds and metal nanoparticles and their role in therapeutics.