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