Table 2.
Screen results of the 2,3-substituted quinoxalin-6-amine analogs.
| Entry | % Growth inhibition at 20μM | ||||||
|---|---|---|---|---|---|---|---|
| A549 | AsPC1 | HT29 | MDA-MB-231 | PC3 | SKOV3 | U2OS | |
| 5a | 23.4 ± 3.3 | 26.2 ± 2.8 | 31.7 ± 2.8 | 25.7 ± 5.1 | 21.8 ± 15.1 | 4.0 ± 3.6 | 31.4 ± 3.6 |
| 5b | 57.8 ± 7.0 | Inactive | 7.6 ± 5.1 | 20.3 ± 5.9 | 57.7 ± 9.4 | 9.0 ± 3.4 | Inactive |
| 5c | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 5d | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 5e | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 5f | 54.6 ± 2.6 | 9.6 ± 6.6 | 52.1 ± 11.6 | 31.3 ± 10.7 | 70.6 ± 1.3 | 24.7 ± 1.1 | 59.6 ± 1.6 |
| 5g | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 5h | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 5i | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 5j | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 5k | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 5l | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 6a | 18.0 ± 0.1 | Inactive | 26.1 ± 15.0 | 19.1 ± 12.5 | 56.8 ± 1.4 | Inactive | 21.4 ± 8.4 |
| 6b | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 6c | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 6d | 19.2 ± 8.9 | Inactive | 42.0 ± 1.9 | 9.0 ± 4.7 | 43.4 ± 9.3 | Inactive | 32.2 ± 0.1 |
| 6e | Inactive | Inactive | 23.9 ± 27.8 | 53.3 ± 7.2 | 19.5 ± 37.4 | Inactive | 50.6 ± 3.9 |
| 6f | 16.6 ± 11.2 | 55.5 ± 25.4 | 81.2 ± 0.7 | 72.6 ± 0.7 | 81.0 ± 8.5 | 55.8 ± 30.7 | 76.1 ± 0.4 |
| 6g | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 6h | 23.3 ± 2.9 | 11.6 ± 4.2 | 16.7 ± 3.7 | 18.2 ± 7.0 | 53.1 ± 9.9 | 16.9 ± 4.9 | 46.5 ± 4.4 |
| 6i | 11.0 ± 1.3 | 29.4 ± 9.8 | Inactive | 16.7 ± 3.9 | 56.9 ± 2.7 | 18.5 ± 4.3 | 54.2 ± 2.2 |
| 6j | 40.3 ± 1.9 | Inactive | 16.3 ± 10.1 | 12.4 ± 5.0 | 30.6 ± 11.6 | 8.9 ± 5.1 | 33.5 ± 0.4 |
| 6k | 93.1 ± 7.8 | >100 | 55.2 ± 4.1 | 90.8 ± 4.5 | >100 | 47.6 ± 2.5 | 80.3 ± 2.4 |
| 6l | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive | Inactive |
| 6m | 39.7 ± 12.8 | Inactive | 19.4 ± 3.6 | 10.9 ± 5.0 | 48.9 ± 7.5 | Inactive | Inactive |
| 7a | >100 | >100 | 74.2 ± 5.2 | 38.4 ± 2.7 | 90.7 ± 4.1 | Inactive | 55.6 ± 6.6 |
| 7b | 99.2 ± 5.2 | 81.1 ± 2.0 | 86.3 ± 7.7 | 92.5 ± 6.6 | 86.4 ± 1.1 | 55.8 ± 24.1 | 87.4 ± 1.1 |
| 7c | >100 | >100 | 88.6 ± 4.6 | >100 | >100 | 94.9 ± 7.9 | >100 |
| 7d | 13.8 ± 9.8 | Inactive | 72.4 ± 7.6 | 50.2 ± 8.9 | 88.5 ± 1.9 | Inactive | 46.9 ± 7.4 |