Table 1.
In vitro activity of N-phenylbenzamide analogs against adult S. mansoni and HEK 293 cells.
| Code | Chemical structure | Adult S. mansoni Severity scores (5 μM)a |
Adult S. mansoni EC50 (μM)b |
HEK 293 CC50 (μM)c |
SId | |||
|---|---|---|---|---|---|---|---|---|
| 1 h | 5 h | 24 h | 48 h | |||||
| 4 |
|
0 | 1 | 1 | 1 | - | > 20 | - |
| 6 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 7 |
|
2 | 2 | 3 | 3 | 3.7 | > 20 | > 5.4 |
| 8 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 9 |
|
3 | 3 | 4 | 4 | 0.08 | 9.8 ± 1.6 | 123 |
| 10 |
|
1 | 1 | 2 | 3 | 1.25 | > 20 | > 16 |
| 11 |
|
3 | 3 | 3 | 4 | 1.10 | 11.1 ± 0.2 | 10.1 |
| 12 |
|
2 | 2 | 2 | 3 | 3.80 | 14.6 ± 2.0 | 3.84 |
| 13 |
|
1 | 1 | 0 | 0 | - | > 20 | - |
| 14 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 15 |
|
1 | 1 | 0 | 0 | - | > 20 | - |
| 16 |
|
1 | 0 | 0 | 0 | - | > 20 | - |
| 17 |
|
1 | 0 | 0 | 0 | - | > 20 | - |
| 18 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 21 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 22 |
|
2 | 2 | 2 | 2 | - | > 20 | - |
| 23 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 24 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 25 |
|
2 | 2 | 2 | 2 | - | > 20 | - |
| 26 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 27 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 28 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 29 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 30 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
| 31 |
|
0 | 0 | 0 | 0 | - | > 20 | - |
a
Each compound was screened twice as a singleton and representative data are shown.
b
24 h time point assay.
c
Human embryonic kidney cell lines; 48 h time point assay.
d
SI, selectivity index, i.e., HEK 293 CC50/WormAssay EC50.