Table 2.
SAR for anti-HCV activity of sophocarpinic acid derivatives.
| Compd. | R | TC50 (μg/mL)a | EC50 (μg/mL)b | SIc |
|---|---|---|---|---|
| 1 | >1000 | 98.04 | >10.2 | |
| 9a | –CH2PhCH3-o | 726.98 | 155.66 | 4.7 |
| 9b | –CH2Ph | >1000 | 49.3 | 20.3 |
| 9c | –CH2PhBr- p | 357.41 | 24.36 | 14.7 |
| 9d | –SO2PhNO2-p | 380.7 | 74.0 | 5.14 |
| 9e | –SO2Ph | >1000 | 257.55 | >3.9 |
| 9f | –SO2PhCH3-p | >1000 | 112.06 | >8.9 |
| 9g | –SO2PhOCH3-p | >1000 | 165.21 | > 6.1 |
| 9h | –SO2PhCF3-p | 530.07 | 7.54 | 70.3 |
| 9i | –SO2PhCl-o | 876.08 | 134.58 | 6.5 |
| 9j | –SO2PhCN-m | 123.08 | 3.98 | 30.9 |
| 9k | –SO2Ph(NHCOCH3)-p | 65.77 | 2.80 | 23.5 |
| 10a | –CH2PhNO2- p | >1000 | 52.82 | >18.9 |
| 10b | –SO2Ph | >1000 | 59.65 | >16.8 |
| 10c | –SO2PhCH3-p | 171.29 | 25.02 | 6.8 |
| 10d | –SO2PhCl-o | 404.64 | 241.27 | 1.68 |
| 10e | –SO2Ph(NHCOCH3)-p | 552.03 | 222.06 | 2.5 |
| 10f | –SO2PhOCH3-p | 700.4 | 291.8 | 2.4 |
| 15 | –CH2Ph | >1000 | >333.3 | 3 |
| RBV | 2000 | 292.46 | 6.84 |
a
Cytotoxic concentration required to inhibit Vero cell growth by 50%.
b
Concentration required to inhibit CVB3 growth by 50%.
c
Selectivity Index values equaled to TC50/EC50.