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  • Title: Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands.
    Author: Cuenca F, Greciano O, Gunaratnam M, Haider S, Munnur D, Nanjunda R, Wilson WD, Neidle S.
    Journal: Bioorg Med Chem Lett; 2008 Mar 01; 18(5):1668-73. PubMed ID: 18243701.
    Abstract:
    A series of tri- and tetra-substituted naphthalene diimides have been designed and synthesized. Several compounds show exceptional affinity for telomeric G-quadruplex DNA in classical and competition FRET assays and SPR studies. They inhibit telomerase in the TRAP assay, and show potent senescence-based short-term anti-proliferative effects on MCF7 and A549 cancer cell lines, and localize in the nucleus and particularly the nucleolus of MCF7 cells.
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