title: Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex.
abstract: 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.
authors.affiliation: Department of Pharmacy, University of Naples "Federico II" Naples, Italy.
authors.forename: Jussara
authors.initials: J
authors.lastname: Amato
authors.affiliation: Department of Pharmacy, University of Naples "Federico II" Naples, Italy.
authors.forename: Nunzia
authors.initials: N
authors.lastname: Iaccarino
authors.affiliation: Department of Pharmacy, University of Naples "Federico II" Naples, Italy.
authors.forename: Bruno
authors.initials: B
authors.lastname: Pagano
authors.affiliation: Department of Pharmacy and Biotechnology (FaBiT), University of Bologna Bologna, Italy.
authors.forename: Rita
authors.initials: R
authors.lastname: Morigi
authors.affiliation: Department of Pharmacy and Biotechnology (FaBiT), University of Bologna Bologna, Italy.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Locatelli
authors.affiliation: Department of Pharmacy and Biotechnology (FaBiT), University of Bologna Bologna, Italy.
authors.forename: Alberto
authors.initials: A
authors.lastname: Leoni
authors.affiliation: Department of Pharmacy and Biotechnology (FaBiT), University of Bologna Bologna, Italy.
authors.forename: Mirella
authors.initials: M
authors.lastname: Rambaldi
authors.affiliation: Experimental Chemotherapy Laboratory, Regina Elena National Cancer Institute Rome, Italy.
authors.forename: Pasquale
authors.initials: P
authors.lastname: Zizza
authors.affiliation: Experimental Chemotherapy Laboratory, Regina Elena National Cancer Institute Rome, Italy.
authors.forename: Annamaria
authors.initials: A
authors.lastname: Biroccio
authors.affiliation: Department of Pharmacy, University of Naples "Federico II" Naples, Italy.
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.affiliation: Department of Pharmacy, University of Naples "Federico II" Naples, Italy.
authors.forename: Antonio
authors.initials: A
authors.lastname: Randazzo
keywords: G-quadruplex; anticancer activity; phenanthroline derivatives; pyridine derivatives; telomeric damage; thermal stabilization
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