title: Antitumour and antimalarial activity of artemisinin-acridine hybrids.
abstract: Artemisinin-acridine hybrids were prepared and evaluated for their in vitro activity against tumour cell lines and a chloroquine sensitive strain of Plasmodium falciparum. They showed a 2-4-fold increase in activity against HL60, MDA-MB-231 and MCF-7 cells in comparison with dihydroartemisinin (DHA) and moderate antimalarial activity. Strong evidence that the compounds induce apoptosis in HL60 cells was obtained by flow cytometry, which indicated accumulation of cells in the G1 phase of the cell cycle.
authors.affiliation: Department of Chemistry, University of Liverpool, Crown Street, Liverpool L69 7ZD, UK.
authors.forename: Michael
authors.initials: M
authors.lastname: Jones
authors.forename: Amy E
authors.initials: AE
authors.lastname: Mercer
authors.forename: Paul A
authors.initials: PA
authors.lastname: Stocks
authors.forename: Louise J I
authors.initials: LJ
authors.lastname: La Pensée
authors.forename: Rick
authors.initials: R
authors.lastname: Cosstick
authors.forename: B Kevin
authors.initials: BK
authors.lastname: Park
authors.forename: Miriam E
authors.initials: ME
authors.lastname: Kennedy
authors.forename: Ivo
authors.initials: I
authors.lastname: Piantanida
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Ward
authors.forename: Jill
authors.initials: J
authors.lastname: Davies
authors.forename: Patrick G
authors.initials: PG
authors.lastname: Bray
authors.forename: Sarah L
authors.initials: SL
authors.lastname: Rawe
authors.forename: Jonathan
authors.initials: J
authors.lastname: Baird
authors.forename: Tafadzwa
authors.initials: T
authors.lastname: Charidza
authors.forename: Omar
authors.initials: O
authors.lastname: Janneh
authors.forename: Paul M
authors.initials: PM
authors.lastname: O'Neill
mesh_terms: D000166:Acridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis; D037621:Artemisinins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle; D045744:Cell Line, Tumor; D004912:Erythrocytes / Q000187:drug effects; D005434:Flow Cytometry; D016193:G1 Phase; D018922:HL-60 Cells; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects
chemical_list: D000166:Acridines; D000962:Antimalarials; D000970:Antineoplastic Agents; D037621:Artemisinins