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

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

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...

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Bibliographic Details
Main Authors: Jussara eAmato, Nunzia eIaccarino, Bruno ePagano, Rita eMorigi, ALESSANDRA eLOCATELLI, ALBERTO eLEONI, Mirella eRambaldi, Pasquale eZizza, Annamaria eBiroccio, Ettore eNovellino, Antonio eRandazzo
Format: Article
Language:English
Published: Frontiers Media S.A. 2014-07-01
Series:Frontiers in Chemistry
Subjects:
Anticancer activity
G-quadruplex
telomeric damage
thermal stabilization
phenanthroline derivatives
pyridine derivatives
Online Access:http://journal.frontiersin.org/Journal/10.3389/fchem.2014.00054/full
Description
Summary: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.
ISSN:2296-2646

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