Table 1. Structures of Hits from the HTS Screen.
P. falciparum strain IC50 a (nM) |
|||||
---|---|---|---|---|---|
compd | EBI code | R1 | 3D7 | W2 | cyotoxicity (μM) Huh7 |
1a | GNF-Pf-5069 | Gly | 63 [460] | 97 [473] | >10 [>100] |
1b | GNF-Pf-5179 | (dl)-Phe | 235 [119] | 271 [122] | >10 [>79] |
1c | GNF-Pf-5466 | (dl)-Leu | 116 [30] | 119 [29] | >10 [42] |
Values are the mean of at least two experiments. Data in brackets are for resynthesized powders; otherwise data are from HTS DMSO stock solutions.