Table 1.
Compound | Helicasea
|
Repliconc,d | |||
---|---|---|---|---|---|
DNA | RNA | ||||
| |||||
IC50(μM)b | IC50(μM)b | EC50 (μM)e | CC50 (μM)f | SI50g | |
UK-1 | 380 | >1200 | 0.77 | 17 | 22 |
1 | >1800 | >1800 | 0.50 | 5.4 | 11 |
2 | >1800 | >1800 | 0.53 | 3.5 | 6.6 |
3 | >1800 | >1800 | 1.4h | 6.3h | 4.5h |
4 | 540 | 590 | 0.53 | 2.5 | 4.7 |
5 | 3.8 | 20 | 2.1 | >20 | >10 |
6 | 2.6 | 20 | 0.54 | >20 | >37 |
Strand separation of radiolabeled oligonucleotides was monitored using gel electrophoresis (see Supplemental Information).
The concentration of compound required to inhibit 50% of helicase activity.
Experiments were carried out at Southern Research Institute, Frederick, MD.
Results are the averages of 2–4 independent dose-response experiments using a combination of luciferase reporter-based and RNA assays unless noted.
The concentration of compound that inhibits 50% of viral RNA replication.
The concentration of compound that kills 50% of the cells.
The ratio of EC50 to CC50.
Result is from a single luciferase reporter-based assay.