Premarineosin A undergoes rapid, chemoselective C12 halogenation under mild conditions, providing brominated, chlorinated, fluorinated, and iodinated analogs. These derivatives retained potent antiplasmodial activity against both chloroquine-sensitive and -resistant Plasmodium falciparum strains and displayed smaller reductions in potency against the resistant strain than the parent compound.
Harris, N. R., Amin, S., Curtis, B. J., Teklemichael, A. A., Dranchak, P., McBride, C. M., Verhey-Henke, L., Warrell, C. J., Dulaney, W. M., Oliphant, E. N., Inglese, J., Su, X.-z., Sherman, D. H., Pereira, F.
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