Design,synthesis and evaluation of 4,5-di-substituted acridone ligands with high G-quadruplex affinity and selectivity,together with low toxicity to normal cells |
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| Authors: | Francisco Cuenca Michael JB Moore Karin Johnson Bérangère Guyen Anne De Cian Stephen Neidle |
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| Institution: | 1. CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, UK;2. Laboratoire de Régulation et Dynamique des Génomes, USM503 INSERM U565, CNRS UMR5153, 75005 Paris, France |
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| Abstract: | A series of 4,5-di-substituted acridones have been designed and synthesized. Several compounds show high affinity for telomeric G-quadruplex DNA in classical and competition FRET assays, together with low duplex DNA affinity, although they do not show activity in a telomerase assay or evidence of telomere shortening. They have low toxicity against a panel of cancer cell lines and a normal human fibroblast line, and produce potent senescence-based long-term growth arrest in the MCF7 and A549 cancer cell lines. |
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