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- W3118820318 abstract "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 two-step 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)." @default.
- W3118820318 created "2021-01-18" @default.
- W3118820318 creator A5039965307 @default.
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- W3118820318 creator A5062229377 @default.
- W3118820318 date "2021-01-13" @default.
- W3118820318 modified "2023-10-17" @default.
- W3118820318 title "PhenQE8, a Novel Ligand of the Human Telomeric Quadruplex" @default.
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- W3118820318 doi "https://doi.org/10.3390/ijms22020749" @default.
- W3118820318 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7828518" @default.
- W3118820318 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33451070" @default.
- W3118820318 hasPublicationYear "2021" @default.
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