Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents |
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| Authors: | Martins Cristina Gunaratnam Mekala Stuart John Makwana Vaidahi Greciano Olga Reszka Anthony P Kelland Lloyd R 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, United Kingdom. |
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| Abstract: | The design, synthesis, biophysical and biochemical evaluation is presented of a new series of benzylamino-substituted acridines as G-quadruplex binding telomerase inhibitors. Replacement of the previously reported anilino substituents by benzylamino groups results in enhanced quadruplex interaction, and for one compound, superior telomerase inhibitory activity. |
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