The ligands showed a clear binding preference for c‐MYC G4 [4e: ΔTm=23.4 °C (ligand concentration 1 μM, ligand:G4=5 : 1), Kd=1.08 μM; Cz1: ΔTm=15.8 °C (ligand concentration 1 μM, ligand:G4=5 : 1), Kd=0.21 μM] and acted as endogenous transcriptional regulators of c‐MYC gene in cancer cells. This evidence concerns the gene MYC and cancer.