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. 2022 Feb 23;13(3):365–370. doi: 10.1021/acsmedchemlett.1c00663

Table 1. In VitroP. falciparum Growth Inhibition of 1a, 13e Stereoisomers, and 7e·HCl.

Compound EC50 (nM)a IPP rescueb
1a 250 ± 70c 100% @ 2.5 μM
(1R,3S)-(−)-13e 1,950 ± 240 50% @ 5 μM
(1S,3S)-(−)-13e 1,300 ± 100 nd
(1S,3R)-(+)-13e 3,690 ± 310 nd
(1R,3R)-(+)-13e 1,430 ± 70 nd
7e·HCl 108 ± 7 0% @ 2.5 μM
a

Growth inhibition (72 h) of asexual blood stages determined using SYBR Green I assay. Values represent average ± SEM from at least three independent biological replicates. The Dd2 strain is resistant to chloroquine, pyrimethamine, and mefloquine.

b

Recovery of parasite growth in the presence of 200 μM IPP, at the indicated concentration of the test compound (Supporting Information); nd designates “not determined”.

c

Reported previously.8