%0 Journal Article
%T Xanthene and Xanthone Derivatives as G-Quadruplex Stabilizing Ligands
%A Alessandro Altieri
%A Antonello Alvino
%A Stephan Ohnmacht
%A Giancarlo Ortaggi
%A Stephen Neidle
%A Daniele Nocioni
%A Marco Franceschin
%A Armandodoriano Bianco
%J Molecules
%D 2013
%I MDPI AG
%R 10.3390/molecules181113446
%X Following previous studies on anthraquinone and acridine-based G-quadruplex ligands, here we present a study of similar aromatic cores, with the specific aim of increasing G-quadruplex binding and selectivity with respect to duplex DNA. Synthesized compounds include two and three-side chain xanthone and xanthene derivatives, as well as a dimeric ¡°bridged¡± form. ESI and FRET measurements suggest that all the studied molecules are good G-quadruplex ligands, both at telomeres and on G-quadruplex forming sequences of oncogene promoters. The dimeric compound and the three-side chain xanthone derivative have been shown to represent the best compounds emerging from the different series of ligands presented here, having also high selectivity for G-quadruplex structures with respect to duplex DNA. Molecular modeling simulations are in broad agreement with the experimental data.
%K G-quadruplex
%K xanthene
%K xanthone
%K ESI-MS
%K FRET
%K telomere
%K c-myc
%K bcl-2
%U http://www.mdpi.com/1420-3049/18/11/13446