TABLE 2.
Antiviral activity against HCMV AD169 and cytotoxicity of K5 derivatives
| Compound | Antiviral activity (EC50, nM)a | Cytotoxicity (CC50, nM)b | SIc |
|---|---|---|---|
| K5 | >833 | >3,333 | >4 |
| K5-NS | >1,667 | >6,667 | >4 |
| K5-OS(L) | >1,785 | >7,142 | >4 |
| K5-OS(H) | >2,227 | >9,090 | >4 |
| K5-N,OS(L) | 76.9 ± 30.8 | >7,690 | >100 |
| K5-N,OS(H) | 12.7 ± 10.1 | >3,333 | >262 |
| Heparin | 28.1 ± 10.7 | >6,667 | >237 |
| GCV | 1,900 ± 200 | 550,000 ± 75,000 | 289 |
a
That is, the compound concentration that inhibits 50% of plaque formation, as determined by modified plaque reduction assays against HCMV AD169 in HFF cells as described in Materials and Methods. Reported values represent the means ± the SD of data derived from at least three independent experiments in performed duplicate.
b
That is, the compound concentration that produces 50% of cytotoxicity, as determined by MTT assays in HFF cells. Reported values represent the means ± the SD of data derived from at least three independent experiments performed in quadruplicate.
c
SI, selectivity index (determined as the ratio between CC50 and EC50).