TABLE 1.
Cytotoxicity and anti-YFV activity of nucleoside analogs
| Compound | Huh-7 cells |
RD cells |
Virus CPE inhibition in RD cells (%) | ||
|---|---|---|---|---|---|
| CC50a (μM) | MNTCa (μM) | CC50a (μM) | MNTCa (μM) | ||
| 1 | >100 | >20 | 56 | >20 | 44.7 ± 0.4 |
| 2 | 81 | >20 | 94 | >20 | 54.3 ± 0.4 |
| 3 | 60 | >20 | >100 | >20 | 26 ± 1.1 |
| 4 | >100 | >20 | 30.9 | >20 | 99.5 ± 0.3 |
| 5 | >100 | >20 | >100 | >20 | <2 |
| 6 | >100 | >20 | >100 | >20 | <5 |
| 7 | >100 | >20 | >100 | >20 | <2 |
| 8 | 37 | >20 | 80 | >20 | <2 |
| 9 | >100 | >20 | >100 | >20 | 95 ± 1 |
| 10 | 70 | >20 | >100 | >20 | 99.5 ± 0.3 |
| 11 | 22 | 15 | >100 | >20 | 99.9 ± 0.1 |
| 12 | >100 | >20 | >100 | >20 | <5 |
| 13 | 17 | >10 | 77 | >20 | 99 ± 0.4 |
| 14 | 10 | 5 | 11 | 7 | 99.8 ± 0.1d |
| 15 | 7 | 5 | 12 | 7.5 | 99.9 ± 0.1d |
| 16b | >100 | >20 | >100 | >20 | 98 ± 0.7 |
| 17 | 2.9 | 2 | 10.5 | 6.5 | 99.5 ± 0.8c |
| 18 | 11.5 | 5.5 | 32.5 | 16 | 90.5 ± 1d |
| 19 | >100 | >20 | >100 | >20 | <5 |
| 20 | 62 | >20 | >100 | >20 | <2 |
| 21 | >100 | >20 | >100 | >20 | 99 ± 0.2 |
a
Cytotoxicity of all nucleoside analogs was measured using MTS assay to calculate the CC50 and maximum nontoxic concentration (MNTC) of each compound.
b
Sofosbuvir (positive control).
c
Compound 17 was tested at 1.5 μM for its anti-YFV activity because of its MNTC.
d
Compounds 14, 15, and 18 were tested in 5 μM for their anti-YFV activity because of their MNTCs. All other compounds were tested in 20 μM against YFV in a CPE inhibition assay using MTS assay.