%0 Journal Article 
%A Gratal Viñuales, Patricia Betsabe
%A González Quero, Julia
%A Pérez Redondo, Adrián
%A Gándara Barreiro, Zoila
%A Gude Rodríguez, Lourdes
%T PhenQE8, a Novel Ligand of the Human Telomeric Quadruplex
%D 2021
%@ 1422-0067
%U http://hdl.handle.net/10017/45847
%X A novel quadruplex ligand based on 1,10-phenanthroline and incorporating two guanyl hydrazone functionalities, PhenQE8, is reported herein. Synthetic access was gained in a twostep procedure with an overall yield of 61%. X-ray diffraction studies revealed that PhenQE8 can adopt an extended conformation that may be optimal to favor recognition of quadruplex DNA.
DNA interactions with polymorphic G-quadruplex telomeric structures were studied by different
techniques, such as Fluorescence resonance energy transfer (FRET) DNA melting assays, circular
dichroism and equilibrium dialysis. Our results reveal that the novel ligand PhenQE8 can efficiently
recognize the hybrid quadruplex structures of the human telomeric DNA, with high binding affinity
and quadruplex/duplex selectivity. Moreover, the compound shows significant cytotoxic activity
against a selected panel of cultured tumor cells (PC-3, HeLa and MCF-7), whereas its cytotoxicity is
considerably lower in healthy human cells (HFF-1 and RPWE-1).
%K 1,10-phenanthroline
%K guanyl hydrazones
%K human telomeric quadruplex
%K DNA interactions
%K antitumor agents
%K Química
%K Chemistry
%~ Biblioteca Universidad de Alcala