Table 1.
SAR Study on A, C and D Rings: EC50s of 1a-v, Compared with 5a
 | ||||
|---|---|---|---|---|
| Compounds | C ring | D ring | ELISA, EC50 (μM) | MTT, CC50 (μM) |
| 5 | - | - | 11.3 ± 3.2 | > 50 |
| 1a |
|
|
4.1 ± 2.1 | > 50 |
| 1b |
|
|
4.7 ± 1.9 | > 50 |
| 1c |
|
|
2.7 ± 1.0 | > 50 |
| 1d |
|
|
2.7 ± 0.7 | > 50 |
| 1e |
|
|
3.0 ± 0.7 | > 50 |
| 1f |
|
|
8.8 ± 3.2 | > 50 |
| 1g |
|
|
34.2 ± 13.6 | > 50 |
| 1h |
|
|
3.2 ± 1.8 | > 50 |
| 1i |
|
|
12.1 ± 3.6 | > 50 |
| 1j |
|
|
5.9 ± 3.3 | > 50 |
| 1k |
|
|
2.1 ± 1.0 | > 50 |
| 1l |
|
|
7.4 ± 1.7 | > 50 |
| 1m |
|
|
46.6 ± 3.2 | > 50 |
| 1n |
|
|
3.0 ± 1.3 | > 50 |
| 1o |
|
|
2.9 ± 0.7 | > 50 |
| 1p |
|
|
5.2 ± 1.9 | > 50 |
| 1q |
|
|
5.7 ± 1.9 | > 50 |
| 1r |
|
|
11.2 ± 2.2 | > 50 |
| 1s |
|
|
2.2 ± 0.5 | > 50 |
| 1t |
|
|
40.8 ± 15.9 | > 50 |
| 1u |
|
|
> 50 | > 50 |
| 1v |
|
|
> 50 | > 50 |
a
EC50: 50% effective concentration, measured by the HBsAg ELISA assay; CC50: 50% cytotoxic concentration, measured by the MTT assay; both CC50 and EC50 are the average of at least two independent determinations.