title: Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
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.
authors.affiliation: CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
authors.forename: Cristina
authors.initials: C
authors.lastname: Martins
authors.forename: Mekala
authors.initials: M
authors.lastname: Gunaratnam
authors.forename: John
authors.initials: J
authors.lastname: Stuart
authors.forename: Vaidahi
authors.initials: V
authors.lastname: Makwana
authors.forename: Olga
authors.initials: O
authors.lastname: Greciano
authors.forename: Anthony P
authors.initials: AP
authors.lastname: Reszka
authors.forename: Lloyd R
authors.initials: LR
authors.lastname: Kelland
authors.forename: Stephen
authors.initials: S
authors.lastname: Neidle
mesh_terms: D000166:Acridines / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001596:Benzylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D004247:DNA / Q000187:drug effects*; D016503:Drug Delivery Systems; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D054856:G-Quadruplexes; D006151:Guanosine; D006801:Humans; D019098:Telomerase / Q000037:antagonists & inhibitors*; D016615:Telomere / Q000187:drug effects*
chemical_list: D000166:Acridines; D000970:Antineoplastic Agents; D001596:Benzylamines; D004791:Enzyme Inhibitors; D006151:Guanosine; D004247:DNA; D019098:Telomerase