title: Synthesis and biological evaluation of extraordinarily potent C-10 carba artemisinin dimers against P. falciparum malaria parasites and HL-60 cancer cells.
abstract: A series of artemisinin dimers incorporating a metabolically stable C-10 carba-linkage have been prepared, several of which show remarkable in vitro antimalarial activity (as low as 30 pM) versus Plasmodium falciparum and in vitro anticancer activity in the micromolar to nanomolar range versus HL-60 cell lines.
authors.affiliation: Department of Chemistry, University of Liverpool, Liverpool, L69 7ZD, UK.
authors.forename: James
authors.initials: J
authors.lastname: Chadwick
authors.forename: Amy E
authors.initials: AE
authors.lastname: Mercer
authors.forename: B Kevin
authors.initials: BK
authors.lastname: Park
authors.forename: Richard
authors.initials: R
authors.lastname: Cosstick
authors.forename: Paul M
authors.initials: PM
authors.lastname: O'Neill
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D019281:Dimerization; D018922:HL-60 Cells; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects
chemical_list: D000962:Antimalarials; D000970:Antineoplastic Agents; D037621:Artemisinins