Table 1.
Compds | R | Antiviral Activity |
Cytotoxicity (μM)d | ||
---|---|---|---|---|---|
HCV (EC50, μM)a | SCV (IC50, μM) |
||||
NTPaseb | Helicasec | ||||
5a | H | >50 | >50 | >50 | >50 |
5b | 3-Cl | 17 | 10 | 40 | >50 |
5c | 4-Cl | 24 | 28 | 53 | >50 |
5d | 3,5-di-Cl | 1 | >50 | >50 | >50 |
5e | 3-I | 4 | 4 | 11 | >50 |
5f | 4-I | 3 | 23 | 31 | >50 |
5g | 3-CN | 17 | 37 | >50 | >50 |
1 | 3-(4-chlorobenzyl-amino) | 0.8 [4] | >50 [7] | 11 [5] | >50 |
3 | 3-NO2 | 5 [7] | >50 | >50 | >50 |
4 | 3-CN | 3 [8] | >50 | >50 | >50 |
Concentration required to inhibit HCV RNA replication by 50% in HCV replicon cell.
Concentration required to inhibit SCV NTPase activity by 50%.
Concentration required to inhibit duplex DNA-unwinding activity of SCV helicase by 50%.
Concentration required to reduce proliferation of normal human fibroblast cell HS27 by 50%.