G-quadruplex ligands have attracted substantial interest recently as potential antineoplastics. The G quadruplex is an appealing nucleic acid drug target, as the G tetrad is structurally distinct from the Watson-Crick base pair. Additionally, the backbone geometries and groove widths differ between G quadruplexes and dsDNA. High-affinity G-quadruplex ligands have begun to show medicinal promise, although the connection between G-quadruplex binding and in vivo activity might not always be obvious. Here, we report novel, high-affinity, high-selectivity G-quadruplex ligands: the azacyanines. We present data comparing the G-quadruplex and Watson-Crick dsDNA binding affinities of these molecules (1). Additionally, we present data related to the binding site for these ligands on the G quadruplex formed by the human telomeric DNA repeat in potassium containing solution.

References and Footnotes

1. Çetinkol ÖP, Engelhart AE, Nanjunda RK, Wilson WD, Hud NV. ChemBioChem 9:1889?1892 (2008).