ArticleInternational journal of molecular sciences2021
PhenQE8, a Novel Ligand of the Human Telomeric Quadruplex.
Article in International journal of molecular sciences, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Taming unconventional nucleic acid structures: synthesis of acridine- and 1,10-phenanthroline-based G-quadruplex binders.RSC advances · 2026Review
- Mono- vs. Bis-Guanyl Hydrazone-Decorated Tricyclic Scaffolds: Effects on G-Quadruplex Binding and Selectivity.International journal of molecular sciences · 2026Article
- A fluorescent probe under the microscope showing dual recognition of B-DNA and G-quadruplex DNA.Communications chemistry · 2026Article
- Aryl Guanyl Hydrazones: A Viable Strategy for Designing BBB-Permeable, Neuroactive Compounds?ACS chemical neuroscience · 2025Review
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Authors and funding
5 authors.
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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).
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