Table 1.
Anti-HCV NS5B RdRp activity of STLC derivatives.
Compound | % Inhibitiona | IC50 (μM)b |
---|---|---|
STLC | 12.6±2.3 | n.d. |
STDC | 17.0±0.6 | n.d. |
NSC123139 | 23.1±1.6 | n.d. |
NSC136870 | 23.4±2.9 | n.d. |
NSC140909 | 30.9±3.7 | n.d. |
NSC123529 | 14.7±1.5 | n.d. |
NSC123138 | 28.3±5.9 | n.d. |
NSC126217 | 20.2±2.5 | n.d. |
1 | 22.4±5.4 | n.d. |
2 | 22.6±2.0 | n.d. |
3 | 36.8±2.4 | n.d. |
4 | 31.2±1.5 | n.d. |
5 | 20.5±1.1 | n.d. |
6 | 36.9±2.5 | n.d. |
7 | 43.5±0.8 | n.d. |
8 | 44.3±3.0 | n.d. |
9 | 60.0±3.4 | 39.7±0.9 |
10 | 17.2±2.9 | n.d. |
11 | 19.1±1.7 | n.d. |
12 | 22.5±2.2 | n.d. |
13 | 34.0±1.1 | n.d. |
14 | 33.1±0.7 | n.d. |
17a | 31.7±1.8 | n.d. |
17b | 28.7±2.1 | n.d. |
17c | 27.4±4.2 | n.d. |
17d | 24.0±4.5 | n.d. |
17e | 36.7±2.1 | n.d. |
17f | 36.0±1.0 | n.d. |
17g | 33.3±2.3 | n.d. |
17h | 28.3±5.9 | n.d. |
17i | 16.1±3.0 | n.d. |
17j | 14.0±3.3 | n.d. |
17k | 22.0±1.4 | n.d. |
17l | n.i. | n.d. |
F-3070 | 82.8±1.3 | 22.3±5.9 |
E-3205 | 40.2±0.7 | n.d. |
F-3065 | 76.7±2.4 | 24.6±6.0 |
Percent inhibition was determined at 100 μM concentration of the indicated compound and represents an average of at least two independent measurements in duplicate.
The IC50 values of the compounds were determined from dose-response curves employing 8–12 concentrations of each compound in duplicate in two independent experiments. Curves were fitted to data points using nonlinear regression analysis and IC50 values were interpolated from the resulting curves using GraphPad Prism 3.03 software.
n.d., not determined.
n.i., no inhibition.