title: Effect of C2-exo unsaturation on the cytotoxicity and DNA-binding reactivity of pyrrolo[2,1-c][1,4]benzodiazepines.
abstract: A series of novel C2-exo unsaturated pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) has been synthesised via a versatile pro-C2 ketone precursor. C2-exo-unsaturation enhances both DNA-binding reactivity and in vitro cytotoxic potency.
authors.affiliation: CRC Gene Targeted Drug Design Research Group, School of Pharmacy and Biomedical Science, University of Portsmouth, Hants, UK.
authors.forename: S J
authors.initials: SJ
authors.lastname: Gregson
authors.forename: P W
authors.initials: PW
authors.lastname: Howard
authors.forename: K E
authors.initials: KE
authors.lastname: Corcoran
authors.forename: S
authors.initials: S
authors.lastname: Barcella
authors.forename: M M
authors.initials: MM
authors.lastname: Yasin
authors.forename: A A
authors.initials: AA
authors.lastname: Hurst
authors.forename: T C
authors.initials: TC
authors.lastname: Jenkins
authors.forename: L R
authors.initials: LR
authors.lastname: Kelland
authors.forename: D E
authors.initials: DE
authors.lastname: Thurston
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D001569:Benzodiazepines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D001570:Benzodiazepinones / Q000737:chemistry; D004247:DNA / Q000378:metabolism*; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D015394:Molecular Structure; D010051:Ovarian Neoplasms; D011758:Pyrroles / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D014407:Tumor Cells, Cultured
chemical_list: D000903:Antibiotics, Antineoplastic; D001570:Benzodiazepinones; D011758:Pyrroles; D001569:Benzodiazepines; C003619:tomaymycin; D004247:DNA