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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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
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spelling doaj-d25f4b2101144987b4970aa596d7e3d62020-11-24T22:26:37ZengFrontiers Media S.A.Frontiers in Chemistry2296-26462014-07-01210.3389/fchem.2014.00054104080Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplexJussara eAmato0Nunzia eIaccarino1Bruno ePagano2Rita eMorigi3ALESSANDRA eLOCATELLI4ALBERTO eLEONI5Mirella eRambaldi6Pasquale eZizza7Annamaria eBiroccio8Ettore eNovellino9Antonio eRandazzo10University of Naples Federico IIUniversity of Naples Federico IIUniversity of Naples Federico IIUniversity of BolognaUniversity of BolognaUniversity of BolognaUniversity of BolognaRegina Elena National Cancer InstituteRegina Elena National Cancer InstituteUniversity of Naples Federico IIUniversity of Naples Federico IIBis-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.http://journal.frontiersin.org/Journal/10.3389/fchem.2014.00054/fullAnticancer activityG-quadruplextelomeric damagethermal stabilizationphenanthroline derivativespyridine derivatives
collection DOAJ
language English
format Article
sources DOAJ
author Jussara eAmato
Nunzia eIaccarino
Bruno ePagano
Rita eMorigi
ALESSANDRA eLOCATELLI
ALBERTO eLEONI
Mirella eRambaldi
Pasquale eZizza
Annamaria eBiroccio
Ettore eNovellino
Antonio eRandazzo
spellingShingle Jussara eAmato
Nunzia eIaccarino
Bruno ePagano
Rita eMorigi
ALESSANDRA eLOCATELLI
ALBERTO eLEONI
Mirella eRambaldi
Pasquale eZizza
Annamaria eBiroccio
Ettore eNovellino
Antonio eRandazzo
Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
Frontiers in Chemistry
Anticancer activity
G-quadruplex
telomeric damage
thermal stabilization
phenanthroline derivatives
pyridine derivatives
author_facet Jussara eAmato
Nunzia eIaccarino
Bruno ePagano
Rita eMorigi
ALESSANDRA eLOCATELLI
ALBERTO eLEONI
Mirella eRambaldi
Pasquale eZizza
Annamaria eBiroccio
Ettore eNovellino
Antonio eRandazzo
author_sort Jussara eAmato
title Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
title_short Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
title_full Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
title_fullStr Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
title_full_unstemmed Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
title_sort bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric g-quadruplex
publisher Frontiers Media S.A.
series Frontiers in Chemistry
issn 2296-2646
publishDate 2014-07-01
description 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.
topic Anticancer activity
G-quadruplex
telomeric damage
thermal stabilization
phenanthroline derivatives
pyridine derivatives
url http://journal.frontiersin.org/Journal/10.3389/fchem.2014.00054/full
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