title: Synthesis and biological evaluation of hybrid acridine-HSP90 ligand conjugates as telomerase inhibitors.
abstract: The synthesis and biological evaluation of a series of bifunctional acridine-HSP90 inhibitor ligands as telomerase inhibitors is herein described. Four hybrid acridine-HSP90 inhibitor conjugates were prepared using a click-chemistry approach, and subsequently shown to display comparable results to the established telomerase inhibitor BRACO-19 in the TRAP-LIG telomerase assay. The conjugates also demonstrated significant cyctotoxity against a number of cancer cell lines, in the sub-μM range.
authors.affiliation: School of Chemistry, University of Nottingham, University Park, NG7 2RD, UK. John.Moses@nottingham.ac.uk.
authors.forename: S
authors.initials: S
authors.lastname: Roe
authors.forename: M
authors.initials: M
authors.lastname: Gunaratnam
authors.forename: C
authors.initials: C
authors.lastname: Spiteri
authors.forename: P
authors.initials: P
authors.lastname: Sharma
authors.forename: R D
authors.initials: RD
authors.lastname: Alharthy
authors.forename: S
authors.initials: S
authors.lastname: Neidle
authors.forename: J E
authors.initials: JE
authors.lastname: Moses
mesh_terms: D000166:Acridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D057930:Click Chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018841:HSP90 Heat-Shock Proteins / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D019098:Telomerase / Q000037:antagonists & inhibitors*
chemical_list: D000166:Acridines; D004791:Enzyme Inhibitors; D018841:HSP90 Heat-Shock Proteins; D008024:Ligands; D019098:Telomerase