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Within the human genome, beyond telomeres, G4 motifs have also been found in promoters, implying a potential role in gene regulation that could be achieved through interactions with small\u2010molecule ligands. In this field, anthraquinone represented a privileged scaffold for the design of G4\u2010targeting molecules. Additionally, emerging evidence proved that compounds bearing two aromatic cores can offer enhanced affinity and selectivity toward G4s due to cooperative binding in a tweezer\u2010like fashion. This study reports the rational design and synthesis of anthraquinone\u2010based building blocks conceived to generate a dimeric ligand connected through a flexible polyethylene glycol (PEG) linker to potentially recognize G4 as molecular tweezers. The interaction of the synthesized compounds with G4 structures has been investigated by biophysical techniques, including fluorescence thermal shift assays, electrospray ionization\u2010mass spectrometry and circular dichroism (CD) spectroscopy, supported by molecular modeling studies. 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