Table 1.
Biological activity of WC-9 analogues against T. gondii (tachyzoites), T. cruzi (amastigotes), and Vero cells.
| Compound |
T. gondii growth EC50 (µM) |
TgFPPS IC50 (µM) |
T. cruzi growth EC50 (µM) |
TcFPPS IC50 (µM) |
HhFPPS IC50 (µM) |
Cytotoxicity EC50 (µM) |
|---|---|---|---|---|---|---|
| 20 | 3.12 ± 0.37 | ND | 7.01 ± 0.51 | ND | ND | >60 |
| 21 | 1.63 ± 0.36 | ND | 5.38 ± 0.82 | ND | ND | >50 |
| 22 | 4.92 ± 1.94 | ND | 5.69 ± 0.47 | ND | ND | >55 |
| 27 | 4.54 ± 0.57 | ND | >10 | ND | ND | >55 |
| 31 | 7.86 ± 0.78 | ND | >10 | ND | ND | >200 |
| 38 | 2.42 ± 0.81 | ND | 11.3 ± 2.5 | ND | ND | 75.7 ± 7.3 |
| 43 | 5.90 ± 0.07 | 0.094 ± 0.020 | >10 | ND | >10 | >100 |
| 48 | > 10.0 | 0.362 ± 0.002 | >20 | 0.8 ± 0.12 | >15 | >200 |
| 53 | 2.40 ± 0.70 | 0.040 ± 0.002 | >10 | >10 | >10 | >50 |
| 58 | 0.67 ± 0.23 | 0.076 ± 0.019 | >10 | ND | >10 | >100 |
| 63 | > 10 | 0.180 ± 0.015 | >10 | 0.32 ± 0.04 | >10.0 | ND |
| 68 | 3.62 ± 0.38 | ND | >10 | ND | ND | ND |
| 73 | 3.13 ± 0.58 | ND | >10 | ND | ND | 7.5 |
| WC-9 | 4.8 ± 0.41[20] | ND | 5.0 ± 1.1[20] | ND | ND | 82.6 ± 7.3 |
| Benznidazole | ND | ND | 1.52 ± 0.10 | ND | ND | ND |
Values are means ± SD of results from at least three independent experiments, n = 3. ND, not determined