Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands |
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| Authors: | Cuenca Francisco Greciano Olga Gunaratnam Mekala Haider Shozeb Munnur Deeksha Nanjunda Rupesh Wilson W David Neidle Stephen |
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| Institution: | CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, UK. |
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| 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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