TABLE 1.
In vitro antimalarial efficacies and cytotoxicities of febrifugine analogs
| Drugs | IC50 (ng/ml)a
|
Selectivity index
|
||||
|---|---|---|---|---|---|---|
| P. falciparum (W2) | P. falciparum (D6) | Neuronal (NG108) cells | Macrophages (J774) cells | NG108, W2 | J744, W2 | |
| Febrifugine | 0.53 ± 0.19 | 0.34 ± 0.08 | 63.5 ± 1.86 | 81 ± 2.13 | 119.81 | 152.83 |
| Halofuginone | 0.145 ± 0.02 | 0.12 ± 0.02 | 177.06 ± 52.5 | 132.25 ± 5.23 | 1,221.12 | 912.05 |
| WR222048 | 0.98 ± 0.26 | 0.82 ± 0.24 | 878.59 ± 198.49 | 498.84 ± 337.32 | 898.81 | 510.33 |
| WR139672 | 1.46 ± 0.27 | 1.23 ± 1.10 | 1,157.36 ± 118.38 | 392.16 ± 72.3 | 791.35 | 268.14 |
| WR092103 | 2.93 ± 0.34 | 2.38 ± 0.05 | 6,864.29 ± 977.14 | 3,605.13 ± 668.51 | 2,346.77 | 1,232.52 |
| WR221232 | 11.54 ± 3.94 | 9.45 ± 1.45 | 7,996.88 ± 1,879.21 | 612.95 ± 310.58 | 692.82 | 53.10 |
| WR140085 | 15.07 ± 2.61 | 12.94 ± 3.03 | 15,479.39 ± 4,184.15 | 425.46 ± 65.26 | 1,027.00 | 28.23 |
| WR090212 | 23.38 ± 1.81 | 18.95 ± 1.65 | 24,820.7 ± 2,193.24 | 2,973.31 ± 490.08 | 1,061.62 | 127.17 |
| WR146115 | 28.73 ± 6.41 | 21.22 ± 2.45 | 67,249.2 ± 15,897.91 | 6,110.63 ± 4,531.51 | 2,340.53 | 212.67 |
| WR059421 | 23.67 ± 2.3 | 17.44 ± 2.82 | 8,933.3 ± 3,186.45 | 492.12 ± 362.21 | 377.37 | 20.79 |
| WR088442 | 245.18 ± 32.77 | 192.8 ± 12.58 | 35,081.2 ± 12,748 | 7,090.2 ± 2,838.04 | 143.09 | 28.92 |
a
Values are means ± standard deviations. All data were collected from three independent experiments, with four replicates in each experiment.