Aryl ethynyl anthraquinones: a useful platform for targeting telomeric G-quadruplex structures

Claudia Percivalle; Claudia Sissi; Maria Laura Greco; Caterina Musetti; Angelica Mariani; Anna Artese; Giosuè Costa; Maria Lucia Perrore; Stefano Alcaro; Mauro Freccero

doi:10.1039/C4OB00220B

Aryl ethynyl anthraquinones: a useful platform for targeting telomeric G-quadruplex structures†

Claudia Percivalle,^a Claudia Sissi,^b Maria Laura Greco,^b Caterina Musetti,^b Angelica Mariani,^a Anna Artese,^c Giosuè Costa,^c Maria Lucia Perrore,^a Stefano Alcaro^c and Mauro Freccero*^a

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^a Dipartimento di Chimica, Università di Pavia, V.le Taramelli 10, Pavia, Italy
E-mail: claudia.percivalle01@universitadipavia.it, angy88@tiscali.it, marialucia.perrone01@universitadipavia.it, mauro.freccero@unipv.it

^b Department of Pharmaceutical and Pharmacological Sciences, v. Marzolo 5, 35131 Padova, Italy
E-mail: claudia.sissi@unipd.it, marialaura.greco@studenti.unipd.it, caterina.musetti@gmail.com

^c Dipartimento di Scienze della Salute, Universitá di Catanzaro, Campus “Salvatore Venuta”, Viale Europa, 88100 Catanzaro, Italy
E-mail: alcaro@unicz.it, artese@unicz.it, gcosta@unicz.it

Abstract

Aryl ethynyl anthraquinones have been synthesized by Sonogashira cross-coupling and evaluated as telomeric G-quadruplex ligands, by the FRET melting assay, circular dichroism, the DNA synthesis arrest assay and molecular docking. Both the binding properties and G-quadruplex vs. duplex selectivity are controlled by the structures of the aryl ethynyl moieties.

Organic & Biomolecular Chemistry

Aryl ethynyl anthraquinones: a useful platform for targeting telomeric G-quadruplex structures†

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Aryl ethynyl anthraquinones: a useful platform for targeting telomeric G-quadruplex structures

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