Table 1.
IC50 of RJF compounds in in-vitro enzyme and cell culture assays of WT and quadruple mutant P. falciparum TS-DHFR
IC50 | in WT DHFR in vitro assay |
in quadruple mutant DHFR in vitro assay |
in WT parasite cell culture |
in quadruple mutant cell culture |
---|---|---|---|---|
RJF 00719 | 21 ± 2 μM | 40 ± 2 μM | 20 ± 2 μM | 19.9 ± 0.5 μM |
RJF 01302 | 29.9 ± 0.5 μM | 39.1 ± 0.5 μM | 22 ± 3 μM | 20 ± 2 μM |
RJF 00670 | 17 ± 2 μM | 20 ± 2 μM | > 50 μM | > 50 μM |