title: Novel C8-linked pyrrolobenzodiazepine (PBD)-heterocycle conjugates that recognize DNA sequences containing an inverted CCAAT box.
abstract: A series of novel DNA-interactive C8-linked pyrrolobenzodiazepine (PBD)-heterocycle polyamide conjugates has been synthesised to explore structure/sequence-selectivity relationships. One conjugate (2d) has a greater selectivity and DNA binding affinity for inverted CCAAT sequences within the Topoisomerase IIα promoter than the known C8-bis-pyrrole PBD conjugate GWL-78 (1b).
authors.affiliation: The School of Pharmacy, University of London, London, UK.
authors.forename: Federico
authors.initials: F
authors.lastname: Brucoli
authors.forename: Rachel M
authors.initials: RM
authors.lastname: Hawkins
authors.forename: Colin H
authors.initials: CH
authors.lastname: James
authors.forename: Geoff
authors.initials: G
authors.lastname: Wells
authors.forename: Terence C
authors.initials: TC
authors.lastname: Jenkins
authors.forename: Tom
authors.initials: T
authors.lastname: Ellis
authors.forename: John A
authors.initials: JA
authors.lastname: Hartley
authors.forename: Philip W
authors.initials: PW
authors.lastname: Howard
authors.forename: David E
authors.initials: DE
authors.lastname: Thurston
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D000951:Antigens, Neoplasm / Q000235:genetics; D001483:Base Sequence; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000235:genetics; D004268:DNA-Binding Proteins / Q000235:genetics; D008958:Models, Molecular; D011401:Promoter Regions, Genetic / Q000235:genetics; D011485:Protein Binding; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000951:Antigens, Neoplasm; D004268:DNA-Binding Proteins; D011758:Pyrroles; D001569:Benzodiazepines; D004250:DNA Topoisomerases, Type II