Tetraplex DNA specific ligands based on the fluorenone-carboxamide scaffold.
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.
Alcaro
Stefano
S
Dipartimento di Scienze Farmacobiologiche Università degli Studi Magna Graecia di Catanzaro, Complesso Ninì Barbieri, 88021 Roccelletta di Borgia (CZ), Italy. alcaro@unicz.it
Artese
Anna
A
Iley
James N
JN
Maccari
Rosanna
R
Missailidis
Sotiris
S
Ortuso
Francesco
F
Ottanà
Rosaria
R
Ragazzon
Patricia
P
Vigorita
Maria Gabriella
MG
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
D005449:Fluorenes; D008024:Ligands; D002244:Carbon; D004247:DNA