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

Table 3. Antimalarial Potencies of 7e·HCl and Its A-/D-Ring Variants.

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Compound R X EC50 (nM)a
7a·HCl CH3 2′,4′-Cl2 583 ± 91
7e·HCl CH3 3′,4′-Cl2 108 ± 7
7f·HCl CH3 H 4,000 ± 900
7g·HCl CH3 4′-Cl 274 ± 12
7h·HCl CH3 3′-Cl 342 ± 7
27e·HCl H 3′,4′-Cl2 227 ± 33
27f·HCl H H 2,500–5,000
27g·HCl H 4′-Cl 496 ± 60
27h·HCl H 3′-Cl 641 ± 11
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.