Table 3. IC50 Values (μM) for the Anti-plasmodial Activity, and Cytotoxicity of Selected Compounds.
|
IC50of Suppression ofP. falciparumproliferation
(μM) |
|||||
|---|---|---|---|---|---|
| Compound | Thiamine-free | [Thiamine] = 2.97 μM | [Thiamine] = 297 μM | HFF Cytotoxicity (μM) | Selectivity Indexa |
| 7ab | 11 ± 4 | 5200 ± 300 | 5500 ± 500 | ND | ND |
| 16a | >200 | >200 | >200 | ND | ND |
| 16b | >200 | >200 | >200 | >200 | ND |
| 16c | 67 ± 5 | 70 ± 8 | 89 ± 19 | 48 ± 5 | 0.7 |
| 17a | 129 ± 9 | 156 ± 13 | 169 ± 11 | >200 | ND |
| 17b | 51 ± 3 | 78 ± 8 | 82 ± 11 | 90 ± 5 | 1.8 |
| 17c | 44 ± 2 | 62 ± 7 | 69 ± 9 | 46 ± 7 | 1.1 |
| 24b | 0.9 ± 0.1 | 1.3 ± 0.2 | 1.4 ± 0.4 | 15 ± 3 | 16.7 |
| 24c | 3.0 ± 1.2 | 3.8 ± 2 | 4.0 ± 1.8 | 44 ± 4 | 14.7 |
a
Selectivity index is IC50 (thiamine-free) vs HFF cytotoxicity; ND, not determined. Refer to Figures S8 and S9 for details.
b
Ref (17).