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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Detalles Bibliográficos
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
Descripción
Sumario: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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