3-alkylthio-1,2,4-triazine dimers with potent antimalarial activity.
We report on the discovery of 3-alkylthio-1,2,4-triazine dimers that are potently toxic to Plasmodium falciparum, with single digit nanomolar activity, and up to several thousand-fold lower toxicity to mammalian cells. They are equipotent against chloroquine-resistant strains of P. falciparum.
Ban
Kung
K
Walter & Eliza Hall Institute of Medical Research, Parkville, Victoria, Australia.
Duffy
Sandra
S
Khakham
Yelena
Y
Avery
Vicky M
VM
Hughes
Andrew
A
Montagnat
Oliver
O
Katneni
Kasiram
K
Ryan
Eileen
E
Baell
Jonathan B
JB
D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy; D008862:Microsomes, Liver / Q000378:metabolism; D010963:Plasmodium falciparum / Q000187:drug effects*; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*
D000962:Antimalarials; D014227:Triazines; C093444:1,2,4-triazine