Table 1. Activity of quinoline and isoquinoline derivatives in in vitro kinase and cell-based assays.
| ||||||
|---|---|---|---|---|---|---|
| Compound | Structures | % inhibition | IC50 (nM) | |||
| EGFR | HER2 | SKBR3 | ||||
| 1 μM | 0.1 μM | 1 μM | 0.1 μM | |||
| 4 | a–e | 90 | 59 | 92 | 62 | 1358 |
| 9a | a–f | 91 | 56 | 92 | 55 | 235 |
| 9b | a–g | 98 | 85 | 95 | 58 | 125 |
| 9c | a–h | 76 | 32 | 80 | 40 | 3199 |
| 9d | a–i | 59 | 22 | 73 | 30 | 4527 |
| 11a | b–d | 69 | 16 | 91 | 50 | 1175 |
| 11b | b–e | 87 | 33 | 86 | 32 | 725 |
| 11c | b–f | 84 | 43 | 77 | 33 | 553 |
| 12a | c–d | 68 | 10 | 92 | 56 | 1389 |
| 12b | c–e | 61 | 9 | 88 | 44 | 610 |
| 12c | c–f | 66 | 15 | 83 | 37 | 392 |
| 14a | c–g | 92 | 54 | 92 | 43 | 103 |
| Lapatinib | 99 | 94 | 96 | 70 | 23 | |