Table 2. In vitro enzymatic kinase assays and anti-proliferative activity of ethynyl-linked isoquinazolines.
| Compound | % inhibition | IC50 (nM) | ||||
|---|---|---|---|---|---|---|
| EGFR | HER2 | SKBR3 | A431 | |||
| 1 μM | 0.1 μM | 1 μM | 0.1 μM | |||
| 13a | 95 | 71 | 95 | 68 | 90 | 850 |
| 13b | 82 | 36 | 88 | 30 | 414 | N.Da |
| 13c | 88 | 49 | 93 | 48 | 567 | N.D |
| 13d | 94 | 73 | 98 | 72 | 125 | N.D |
| 13e | 74 | 29 | 88 | 28 | 427 | N.D |
| 13f | 98 | 89 | 96 | 81 | 12 | 414 |
| Lapatinib | 99 | 94 | 96 | 70 | 23 | 418 |
N.D: not determined.