Table 5.
IC50 values of compounds 6c, 6i, 10a and 11a against DENV/ZIKV polymerases and MTases.
| Cpds. | IC50 (μM)a |
IC50 (μM)a |
|||
|---|---|---|---|---|---|
| D2polb | D2 NS5c | ZIKV NS5d | DENV NS5-MTase | ZIKV NS5-MTase | |
| 6c | 31.2 ± 7.8 | >100 | 18.9 ± 3.1 | NA | NA |
| 6i | 20.8 ± 5.7 | 43.7 ± 12.0 | 12.8 ± 2.2 | 112.0 ± 51.5 | NA |
| 10a | >100 | 153.2 ± 38.2 | 105 ± 24.3 | NA | NA |
| 11a | >100 | >100 | >100 | 226.1 ± 107.4 | NA |
| 3'dATP control | 0.27 ± 0.03 | 0.32 ± 0.05 | 1 ± 0.2 | – | – |
| Sinefungin | – | – | – | (0,63 ± 0,04)52 | (1,18 ± 0,05)53 |
a
inhibition concentration 50%.
b
D2pol: polymerase domain of dengue 2 virus.
c
D2 NS5: full length DENV protein.
d
ZIKV NS5: full length ZIKV protein. Literature data for Sinefungin are reported in parenthesis.