TABLE 2.
Inhibitory effects of the 14 lead compounds against binding of NVs to the corresponding HBGAs
| Compounda | EC50b (μM) for the following virus and HBGA:
|
CC50c (μM) | |||||||
|---|---|---|---|---|---|---|---|---|---|
| rVA387
|
rNorwalk
|
rVA207
|
rMOH
|
||||||
| A | B | H | A | H | Le | A | B | ||
| 1 | 2.2 | 5.8 | 6.8 | 15.6 | 18.9 | >100 | >100 | >100 | 158.0 |
| 2 | 4.8 | 18.6 | 11.9 | 22.9 | 24.5 | >100 | 16.5 | 13.3 | 78.6 |
| 3 | 7.8 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | 82.7 |
| 4 | 8.1 | 13.1 | 14.2 | 14.1 | 22.6 | >100 | >100 | >100 | 112.6 |
| 5 | 9.1 | 13.5 | 7.2 | 18.2 | 36.3 | >100 | >100 | >100 | 46.7 |
| 6 | 9.3 | 44.6 | 41.1 | >100 | >100 | >100 | >100 | >100 | 52.7 |
| 7 | 9.6 | 26.0 | 7.6 | >100 | >100 | >100 | >100 | >100 | 323.6 |
| 8 | 10.9 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | 157.3 |
| 9 | 11.7 | >100 | 47.5 | >100 | >100 | >100 | >100 | >100 | 40.3 |
| 10 | 11.8 | 7.9 | 7.5 | 35.0 | 19.8 | >100 | >100 | >100 | 220.3 |
| 11 | 12.8 | 35.3 | 26.1 | >100 | >100 | >100 | >100 | >100 | 262.8 |
| 12 | 12.8 | 32.5 | 28.2 | 53.0 | 47.8 | >100 | >100 | >100 | 180.2 |
| 13 | 13.6 | 49.5 | 48.1 | >100 | >100 | >100 | >100 | >100 | 70.6 |
| 14 | 13.7 | >100 | >100 | >100 | >100 | >100 | >100 | >100 | 12.3 |
a
The solubilities of compounds 1 to 8 and of compounds 10 to 13 are greater than 400 μM; the solubilities of compounds 9 and 14 are greater than 100 μM.
b
Effective concentration required to achieve 50% inhibition of the binding of a norovirus to the corresponding HBGA. Experiments were repeated three times; the data in the table are the average EC50s.
c
The concentration of a compound that causes 50% inhibition of cell growth. Experiments were repeated three times; the data in the table are the average CC50s.