Table 1.
Effective concentration (EC50), cytotoxic concentration (CC50), and selectivity index (SI50) of compounds (1–28) tested on Hepatitis C virus (HCV) genotype (GT) 1b replicons.
| Code | R | Stereo-Chemistry * | R΄ | HCV Replicon 1b | ||
|---|---|---|---|---|---|---|
| ||||||
| 1 |
|
S | -CH3 |
EC
50
(nM) |
CC
50
(nM) |
SI 50 a |
| 2 |
|
S | -CH2CH3 | >1000 | >100,000 | ND b |
| 3 |
|
S | -C4H9 | >1000 | >100,000 | ND |
| 4 |
|
S | -CH2C6H5 | 966.90 | >100,000 | >103 |
| 5 |
|
R | -CH3 | 801.40 | >100,000 | >125 |
| 6 |
|
R | -CH2CH3 | 102 | 79,550 | 780 |
| 7 |
|
R | -C4H9 | 981.40 | >100,000 | >102 |
| 8 |
|
R | -CH2C6H5 | 45.42 | >100,000 | >2202 |
| 9 |
|
S | -CH3 | 27.50 | >100,000 | >3636 |
| 10 |
|
S | -CH2CH3 | 0.137 | 85,510 | 622,344 |
| 11 |
|
S | -C4H9 | 976.60 | 65,950 | 68 |
| 12 |
|
S | -CH2C6H5 | >1000 | 46,450 | ND |
| 13 |
|
R | -CH3 | 0.081 | >100,000 | >1,238,850 |
| 14 |
|
R | -CH2CH3 | 2.55 | >100,000 | >39,185 |
| 15 |
|
R | -C4H9 | >1000 | 34,220 | ND |
| 16 |
|
R | -CH2C6H5 | >1000 | >100,000 | ND |
| 17 |
|
S | -CH3 | 10.66 | >100,000 | >9381 |
| 18 |
|
S | -CH2CH3 | 150.60 | >100,000 | >664 |
| 19 |
|
S | -C4H9 | >1000 | >100,000 | ND |
| 20 |
|
S | -CH2C6H5 | >1000 | 98,730 | ND |
| 21 |
|
S | -CH3 | 8.50 | 87,510 | 10,298 |
| 22 |
|
S | -CH2CH3 | 7.49 | >100,000 | >13,349 |
| 23 |
|
S | -C4H9 | 2.25 | >100,000 | >44,444 |
| 24 |
|
S | -CH2C6H5 | 1.12 | >100,000 | >89,606 |
| 25 |
|
R | -CH3 | 0.142 | 95,390 | 669,874 |
| 26 |
|
R | -CH2CH3 | 0.036 | >100,000 | >2,779,322 |
| 27 |
|
R | -C4H9 | 4.03 | >100,000 | >24,795 |
| 28 |
|
R | -CH2C6H5 | 94.55 | >100,000 | >1,058 |
| Daclatasvir | --- | --- | --- | 0.027 | 17,700 | 655,556 |
| IV | --- | --- | --- | >1000 | 44990 | ND |
a SI50 = CC50/EC50; b ND: Not Determined; * absolute configuration of terminal AA.