Table 3.
In vitro activity of analogues 47–55.
 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| No | R | PARP1 enzyme IC50 (nmol/L) | Cell activity IC50 (nmol/L)a | No | R | PARP1 enzyme IC50 (nmol/L) | Cell activity IC50 (nmol/L)a | ||
| V-C8 (BRCA2−/−) | V79 (BRCA2+/+) | V-C8 (BRCA2−/−) | V79 (BRCA2+/+) | ||||||
| 1 | 7.3±0.5 | 263.6 | >10000 | ||||||
| 43 |
|
2.7±0.6 | 37.6 | 2737.8 | 50 |
|
2.2±1.3 | 3.2 | 1632.9 |
| 44 |
|
4.6±2.3 | 41.9 | 978.6 | 51 |
|
14.8±4.8 | ||
| 45 |
|
27.9±7.8 | 52 |
|
23.1±7.1 | ||||
| 46 |
|
9.1±4.5 | 774.8 | >10000 | 53 |
|
33.7±14.2 | ||
| 47 |
|
4.4±2.1 | 9.6 | 385.1 | 54 |
|
1.6±0.7 | 615.6 | >10000 |
| 48 |
|
3.9±2.1 | 115.1 | 3481.6 | 55 |
|
4.3±1.8 | 267.0 | 2662.1 |
| 49 |
|
33.9±15.7 | |||||||
