Naphthalimide derivs. were designed and the synthesis of the target compds. was achieved using as a suitable reactant 5,8-diamino-1H,3H-naphtho[1,8-cd]pyran-1,3-dione. Selectivity for quadruplex DNA binding and stabilization by a set of compds. were explored through two different methods (UV absorption and thermal denaturation). Quadruplex DNA interaction of the above-mentioned naphthalimides [i.e., N,N'-[2,3-dihydro-1,3-dioxo-1H-benz[de]isoquinoline-5,8-diyl]bis[1-pyrrolidinepropanamide] derivs.] was further characterized by an NMR study. Quantification of relative quadruplex and duplex binding affinity consts. puts some of these ligands among the most selective quadruplex DNA interactive agents reported to date.
Trisubstituted naphthalimides for DNA quadruplex binding selectivity: synthesis, NMR and biophysical studies / A., Peduto; R., Filosa; C., Petronzi; S., Missailidis; P., Ragazzon; S., Smith; Esposito, Veronica; Virgilio, Antonella; Galeone, Aldo. - (2009), pp. 45-52. (Intervento presentato al convegno Joint Meeting on Medicinal Chemistry: Hungarian-Austrian-Czech-German-Greek-Italian-Polish-Slovak-Slovenian tenutosi a Budapest, Ungheria nel 24-27 Giugno 2009).
Trisubstituted naphthalimides for DNA quadruplex binding selectivity: synthesis, NMR and biophysical studies
ESPOSITO, VERONICA;VIRGILIO, ANTONELLA;GALEONE, ALDO
2009
Abstract
Naphthalimide derivs. were designed and the synthesis of the target compds. was achieved using as a suitable reactant 5,8-diamino-1H,3H-naphtho[1,8-cd]pyran-1,3-dione. Selectivity for quadruplex DNA binding and stabilization by a set of compds. were explored through two different methods (UV absorption and thermal denaturation). Quadruplex DNA interaction of the above-mentioned naphthalimides [i.e., N,N'-[2,3-dihydro-1,3-dioxo-1H-benz[de]isoquinoline-5,8-diyl]bis[1-pyrrolidinepropanamide] derivs.] was further characterized by an NMR study. Quantification of relative quadruplex and duplex binding affinity consts. puts some of these ligands among the most selective quadruplex DNA interactive agents reported to date.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
