title: Tetraplex DNA specific ligands based on the fluorenone-carboxamide scaffold.
abstract: A series of fluorenone-carboxamide compounds was analyzed with regard to DNA binding properties by UV spectroscopy and competition dialysis methods. The morpholino derivative 10 provided interesting results in terms of affinity and specificity toward the DNA G-tetraplex structures. Interactions against this target were evaluated by a comparative molecular modeling study in agreement with the experimental data, proposing a model for the rational design of new agents with potent and selective DNA tetraplex binding properties.
authors.affiliation: Dipartimento di Scienze Farmacobiologiche Università degli Studi Magna Graecia di Catanzaro, Complesso Ninì Barbieri, 88021 Roccelletta di Borgia (CZ), Italy. alcaro@unicz.it
authors.forename: Stefano
authors.initials: S
authors.lastname: Alcaro
authors.forename: Anna
authors.initials: A
authors.lastname: Artese
authors.forename: James N
authors.initials: JN
authors.lastname: Iley
authors.forename: Rosanna
authors.initials: R
authors.lastname: Maccari
authors.forename: Sotiris
authors.initials: S
authors.lastname: Missailidis
authors.forename: Francesco
authors.initials: F
authors.lastname: Ortuso
authors.forename: Rosaria
authors.initials: R
authors.lastname: Ottanà
authors.forename: Patricia
authors.initials: P
authors.lastname: Ragazzon
authors.forename: Maria Gabriella
authors.initials: MG
authors.lastname: Vigorita
mesh_terms: D001667:Binding, Competitive; D002244:Carbon / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004247:DNA / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005449:Fluorenes / Q000737:chemistry*; D007700:Kinetics; D008024:Ligands; D008956:Models, Chemical; D008968:Molecular Conformation; D013056:Spectrophotometry, Ultraviolet; D016615:Telomere / Q000648:ultrastructure; D013816:Thermodynamics; D014466:Ultraviolet Rays
chemical_list: D005449:Fluorenes; D008024:Ligands; D002244:Carbon; D004247:DNA