Recently, NiII and ZnII metal complexes of the ligand Salpyrim have been synthesized and characterized. Their affinity for wild-type h-Telo G-quadruplex DNA and for calf thymus DNA was investigated by UV absorption spectroscopy, circular dichroism and viscometry. The data collectively suggest that both complexes bind effectively to G-quadruplexes by direct end-stacking, stabilizing the oligonucleotide secondary structure. The two complexes are also typical B-DNA intercalators. Remarkably, their binding constants, Kb, with the G4s structures are about 10 fold higher than those with B-DNA, highlighting the selectivity. Experiments to evaluate the biological activity of the two complexes against MCF7 and HeLa cancer cell lines are currently ongoing.
Marrone, A., Bonsignore, R., Terenzi, A., Spinello, A., Gentile, C., Martorana, A., et al. (2014). NiII, and ZnII Schiff Base Complexes: Telomeric G-quadruplex Stabilizers. In Congresso: Ricerca di base, interdisciplinare e traslazionale in ambito Biologico e Biotecnologico (II ed.) 26 e 27 Giugno 2014 Aula Mutolo della Sezione di Biologia Cellulare del Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF).
NiII, and ZnII Schiff Base Complexes: Telomeric G-quadruplex Stabilizers
Bonsignore, Riccardo;TERENZI, Alessio;SPINELLO, Angelo;GENTILE, Carla;MARTORANA, Annamaria;ALMERICO, Anna Maria;LAURIA, Antonino;BARONE, Giampaolo
2014-01-01
Abstract
Recently, NiII and ZnII metal complexes of the ligand Salpyrim have been synthesized and characterized. Their affinity for wild-type h-Telo G-quadruplex DNA and for calf thymus DNA was investigated by UV absorption spectroscopy, circular dichroism and viscometry. The data collectively suggest that both complexes bind effectively to G-quadruplexes by direct end-stacking, stabilizing the oligonucleotide secondary structure. The two complexes are also typical B-DNA intercalators. Remarkably, their binding constants, Kb, with the G4s structures are about 10 fold higher than those with B-DNA, highlighting the selectivity. Experiments to evaluate the biological activity of the two complexes against MCF7 and HeLa cancer cell lines are currently ongoing.File | Dimensione | Formato | |
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