Table 1.
In vitro T. gondii growth inhibition and cytotoxicity on HeLa cells.
| Compounds | R | IC50a in HeLa cells (μM) | IC50b in T. gondii (μM) | SIc |
|---|---|---|---|---|
| 1a | -H | >1000 | >1000 | – |
| 1b | 2-F | 419.6 | 711.9 | 0.59 |
| 1c | 3-F | >1000 | >1000 | – |
| 1d | 4-F | >1000 | >1000 | – |
| 1e | 2-Cl | 466.1 | 239.6 | 1.95 |
| 1f | 3,4-Cl | 408.0 | 462.1 | 0.88 |
| 1g | 2-Br | 240.4 | 301.7 | 0.80 |
| 1h | 2-I | 230.4 | 273.8 | 0.84 |
| 1i | 2-OCH3 | >1000 | >1000 | – |
| 1j | 3,4,5-OCH3 | 353.7 | 301.3 | 1.17 |
| 2a | -H | 836.8 | >1000 | – |
| 2b | 4-Cl | 328.7 | >1000 | – |
| 2c | 4-OCH3 | >1000 | >1000 | – |
| 2d | 4-CH3 | >1000 | >1000 | – |
| 2e | 3,4-Cl | >1000 | >1000 | – |
| 3a | -H | 101.5 | 88.0 | 1.15 |
| 3b | 4-Cl | 2.4 | 6.7 | 0.36 |
| 3c | 4-F | 88.2 | 61.4 | 1.44 |
| 3d | 4-NO2 | 226.7 | 128.0 | 1.77 |
| 3e | 4-OCH3 | 78.2 | 116.5 | 0.67 |
| Spiramycin | – | 189.0 | 262.2 | 0.72 |
| Ursolic Acid | – | 44.8 | 72.2 | 0.62 |
a
IC50 in HeLa cells: Median toxicity dose, a measure of cytotoxicity against host cells.
b
IC50 in T. gondii: Median inhibitory concentration, a measure of tachyzoite inhibition.
c
SI: Selectivity index, a measure of efficacy, calculated by IC50 in HeLa cells/IC50 in T. gondii.