AUTHOR=Amato Jussara , Iaccarino Nunzia , Pagano Bruno , Morigi Rita , Locatelli Alessandra , Leoni Alberto , Rambaldi Mirella , Zizza Pasquale , Biroccio Annamaria , Novellino Ettore , Randazzo Antonio 

TITLE=Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex

JOURNAL=Frontiers in Chemistry

VOLUME=Volume 2 - 2014

YEAR=2014

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2014.00054

DOI=10.3389/fchem.2014.00054

ISSN=2296-2646

ABSTRACT=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.