Antitumour and antimalarial activity of artemisinin-acridine hybrids.
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.
Jones
Michael
M
Department of Chemistry, University of Liverpool, Crown Street, Liverpool L69 7ZD, UK.
Mercer
Amy E
AE
Stocks
Paul A
PA
La Pensée
Louise J I
LJ
Cosstick
Rick
R
Park
B Kevin
BK
Kennedy
Miriam E
ME
Piantanida
Ivo
I
Ward
Stephen A
SA
Davies
Jill
J
Bray
Patrick G
PG
Rawe
Sarah L
SL
Baird
Jonathan
J
Charidza
Tafadzwa
T
Janneh
Omar
O
O'Neill
Paul M
PM
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
D000166:Acridines; D000962:Antimalarials; D000970:Antineoplastic Agents; D037621:Artemisinins