Table 1.
IC50 values (μM) of kinase inhibition, A431 cytotoxicity and inhibition of the CAM assay
| R | EGFR kinase | VEGFR-2 kinase | PDGFRβ kinase | A431 cytotoxicity | CAM angiogenesis | |
|---|---|---|---|---|---|---|
| 1 | H | >200 | 171.2±18.0 | 43.1±4.7 | 4.9±0.7 | 50.8±6.7 |
| 2 | 2-CH(CH3)2 | >200 | >200 | 21.7±2.6 | 126.4±18.0 | 2.12±0.18 |
| 3 | 4-CH(CH3)2 | 42.6±5.8 | 11.0±1.8 | 7.8±0.9 | 126.4±13.9 | 14.8±1.6 |
| 4 | 3-F | >300 | 55.7±7.0 | 7.1±1.0 | 9.8±1.3 | 78.3±8.3 |
| 5 | 4-F | 276.1±30.2 | 89.3±9.2 | 5.9±0.7 | 50.3±7.0 | 46.7±5.9 |
| 6 | 3-Cl | 19.6±2.7 | 133.9±16.8 | >500 | 235.0±29.1 | ND |
| 7 | 4-Cl | 26.0±3.2 | >200 | 0.8±0.08 | 9.7±1.1 | 0.82±0.09 |
| 8 | 3-Br | 24.1±3.1 | >200 | 126.3±15.0 | >500 | 104.3±14.2 |
| 9 | 4-Br | >300 | 30.1±4.8 | 38.9±4.0 | 103.1±14.8 | 19.1±2.0 |
| 10 | 4-CF3 | >300 | >200 | 23.1±0.38 | 306.3±40.1 | 8.1±1.4 |
| 11 | 3-OCH3 | >200 | 43.0±5.9 | 75.5±9.1 | 13.9±1.6 | 36.4±3.9 |
| 12 | 4-F,3-Cl | >200 | 72.9±0.9 | 6.4±0.7 | 158.1±17.9 | ND |
| 13 | 2-F, 4-Cl | 11.7±2.1 | 197.1±2.6 | 3.6±0.6 | 9.7±0.8 | 3.67±0.4 |
| 18 | 0.23±0.03 | |||||
| 19 | 3.75±0.06 | |||||
| semaxanib | 12.9±2.7 | 0.04±0.009 | ||||
| sunitinib | 172.1±19.4 | 18.9±2.7 | 83.1±10.1 | |||
| erlotinib | 1.2±0.2 | 124.7±18.2 | 12.2±1.9 | |||
| cisplatin | 10.6±2.9 |
ND. Not determined.