Table 2.
Activity in enzyme assays | |||||||||
---|---|---|---|---|---|---|---|---|---|
IN IC50 (μM)a | RNaseH | Antiviral activity and cytotoxicity | |||||||
R | X | 3’-P | ST | % in. at 10 μMb | IC50 (μM)x | EC50(μM)c | CC50 (μM)d | SIe | |
10x | Et | >333 | 120 | 19.4 | nd | >50 | ndf | ||
10y | Et | >333 | 32 | 29.7 | nd | >50 | nd | ||
10z | Et | >333 | 14 | −5.6 | nd | >50 | nd | ||
10aa | Et | >1000 | 3.5 | 4.4 | nd | >50 | nd | ||
11x | H | >333 | <0.45 | 33.0 | nd | >50 | nd | ||
11y | H | 18 | <0.45 | 40.7 | nd | 4.8 | >50 | >10.4 | |
11z | H | >1000 | 16 | −2.6 | nd | >50 | nd | ||
11aa | H | 70 | 0.40 | 16.4 | nd | >50 | nd |
Inhibitory concentration 50% (μM) determined from dose response curves.
Percentage of inhibition determined at compound concentration of 10 μM.
Effective concentration 50% (μM).
Cytotoxic concentration 50% (μM).
SI = CC50/EC50.
nd: not determined.