title: Antimalarial benzo[c]phenanthridines.
abstract: Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC(50) below 5ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC(50) below 30ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.
authors.affiliation: Department of Pharmaceutical Sciences, University of Strathclyde, 27 Taylor Street, Glasgow, G4 0NR Scotland, UK.
authors.forename: James M
authors.initials: JM
authors.lastname: Nyangulu
authors.forename: Samantha L
authors.initials: SL
authors.lastname: Hargreaves
authors.forename: Susan L
authors.initials: SL
authors.lastname: Sharples
authors.forename: Simon P
authors.initials: SP
authors.lastname: Mackay
authors.forename: Roger D
authors.initials: RD
authors.lastname: Waigh
authors.forename: Olivier
authors.initials: O
authors.lastname: Duval
authors.forename: Eddie K
authors.initials: EK
authors.lastname: Mberu
authors.forename: William M
authors.initials: WM
authors.lastname: Watkins
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008826:Microbial Sensitivity Tests; D009429:Netropsin / Q000737:chemistry / Q000494:pharmacology; D010617:Phenanthridines / Q000737:chemistry* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000502:physiology
chemical_list: D000962:Antimalarials; D010617:Phenanthridines; C404513:ethoxidine; D009429:Netropsin