Bis-indolinone derivatives having either2,6-disubstituted pyridine core(1a and1b) 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.
Jussara Amato, Nunzia Iaccarino, Bruno Pagano, Rita Morigi, Alessandra Locatelli, Alberto Leoni, et al. (2014). Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex. FRONTIERS IN CHEMISTRY, 2, 1-8 [10.3389/fchem.2014.00054].
Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex.
MORIGI, RITA;LOCATELLI, ALESSANDRA;LEONI, ALBERTO;RAMBALDI, MIRELLA;
2014
Abstract
Bis-indolinone derivatives having either2,6-disubstituted pyridine core(1a and1b) 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
