Fig. 5: Diversifying the (−)-premarineosin A (3) scaffold improved selectivity against Plasmodium falciparum.

Compounds were tested against 3D7 (chloroquine-sensitive) and Dd2 (chloroquine-resistant) P. falciparum strains for antimalarial activity and the HEK293 embryonic kidney and MOLT4 T-cell leukemia cell lines for cytotoxicity to mammalian cell lines. Selectivity Index = EC50 Mammalian Cell Line / EC50 P. falciparum.