%0 Journal Article
%T Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
%A Jussara Amato
%A Nunzia Iaccarino
%A Bruno Pagano
%A Rita Morigi
%A Alessandra Locatelli
%A Alberto Leoni
%A Mirella Rambaldi
%A Pasquale Zizza
%A Annamaria Biroccio
%A Ettore Novellino
%A Antonio Randazzo
%J Frontiers in Chemistry
%D 2014
%I Frontiers Media
%R 10.3389/fchem.2014.00054
%X Bis-indolinone derivatives having either 2,6-disubstituted pyridine core (1a and 1b) or 1,10-disubstituted phenanthroline core (2a and 2b), already known to have antitumor activity, have been tested as potential G-quadruplex binders. Compounds 2a and 2b are able to selectively stabilize G-quadruplex over duplex DNA, and also to discriminate among different G-quadruplex structures, having a particular affinity for the parallel form of the human telomeric G-quadruplex. Both compounds are also able to induce telomeric DNA damage that may explain the activity of these compounds.
%K G-quadruplex
%K anticancer activity
%K telomeric damage
%K thermal stabilization
%K phenanthroline derivatives
%K pyridine derivatives
%U http://www.frontiersin.org/Journal/10.3389/fchem.2014.00054/abstract