title: Human telomerase inhibition by substituted acridine derivatives.
abstract: A series of 3,6-disubstituted acridine derivatives have been rationally designed as telomerase inhibitors. They have been designed on the basis that inhibition of telomerase occurs by stabilising G-quadruplex structures formed by the folding of telomeric DNA. The most potent inhibitors have IC50 values against telomerase of between 1.3 and 8 microM, comparable to their cytotoxicity in ovarian cancer cell lines.
authors.affiliation: CRC Biomolecular Structure Unit, The Institute of Cancer Research, Sutton, Surrey, UK.
authors.forename: R J
authors.initials: RJ
authors.lastname: Harrison
authors.forename: S M
authors.initials: SM
authors.lastname: Gowan
authors.forename: L R
authors.initials: LR
authors.lastname: Kelland
authors.forename: S
authors.initials: S
authors.lastname: Neidle
mesh_terms: D000166:Acridines / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D019098:Telomerase / Q000037:antagonists & inhibitors*; D014407:Tumor Cells, Cultured
chemical_list: D000166:Acridines; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D019098:Telomerase