Synthesis and biological evaluation of extraordinarily potent C-10 carba artemisinin dimers against P. falciparum malaria parasites and HL-60 cancer cells.
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.
Chadwick
James
J
Department of Chemistry, University of Liverpool, Liverpool, L69 7ZD, UK.
Mercer
Amy E
AE
Park
B Kevin
BK
Cosstick
Richard
R
O'Neill
Paul M
PM
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
D000962:Antimalarials; D000970:Antineoplastic Agents; D037621:Artemisinins