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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Autores principales: Amato, Jussara, Iaccarino, Nunzia, Pagano, Bruno, Morigi, Rita, Locatelli, Alessandra, Leoni, Alberto, Rambaldi, Mirella, Zizza, Pasquale, Biroccio, Annamaria, Novellino, Ettore, Randazzo, Antonio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2014
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109613/
https://www.ncbi.nlm.nih.gov/pubmed/25105115
http://dx.doi.org/10.3389/fchem.2014.00054
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author Amato, Jussara
Iaccarino, Nunzia
Pagano, Bruno
Morigi, Rita
Locatelli, Alessandra
Leoni, Alberto
Rambaldi, Mirella
Zizza, Pasquale
Biroccio, Annamaria
Novellino, Ettore
Randazzo, Antonio
author_facet Amato, Jussara
Iaccarino, Nunzia
Pagano, Bruno
Morigi, Rita
Locatelli, Alessandra
Leoni, Alberto
Rambaldi, Mirella
Zizza, Pasquale
Biroccio, Annamaria
Novellino, Ettore
Randazzo, Antonio
author_sort Amato, Jussara
collection PubMed
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.
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spelling pubmed-41096132014-08-07 Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex Amato, Jussara Iaccarino, Nunzia Pagano, Bruno Morigi, Rita Locatelli, Alessandra Leoni, Alberto Rambaldi, Mirella Zizza, Pasquale Biroccio, Annamaria Novellino, Ettore Randazzo, Antonio Front Chem Chemistry 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. Frontiers Media S.A. 2014-07-24 /pmc/articles/PMC4109613/ /pubmed/25105115 http://dx.doi.org/10.3389/fchem.2014.00054 Text en Copyright © 2014 Amato, Iaccarino, Pagano, Morigi, Locatelli, Leoni, Rambaldi, Zizza, Biroccio, Novellino and Randazzo. http://creativecommons.org/licenses/by/3.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Chemistry
Amato, Jussara
Iaccarino, Nunzia
Pagano, Bruno
Morigi, Rita
Locatelli, Alessandra
Leoni, Alberto
Rambaldi, Mirella
Zizza, Pasquale
Biroccio, Annamaria
Novellino, Ettore
Randazzo, Antonio
Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex
title 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_short 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
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109613/
https://www.ncbi.nlm.nih.gov/pubmed/25105115
http://dx.doi.org/10.3389/fchem.2014.00054
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