Table 3.
VEGFR2/FGFR1/PDGFRβ inhibition of the typical compounds C1–C41 obtained by R3 group optimization.
| Compd. | Structure or R3 | IC50 (nmol/L) |
||
|---|---|---|---|---|
| VEGFR2 | FGFR1 | PDGFRβ | ||
| Lead compd. |  |
9.4 | 188.0 | 143.0 |
| C1 |  |
32.7 | 436.4 | 77.2 |
| C2 |  |
78.6 | 63.0 | 311.1 |
| C3 |  |
10.0 | 129.9 | 84.3 |
| C4 |  |
22.6 | 378.4 | 139.9 |
| C5 |  |
30.1 | 645.7 | 78.5 |
| C6 |  |
110.3 | 634.7 | 89.1 |
| C7 |  |
55.1 | 415.9 | 80.1 |
| C8 |  |
59.7 | 1216.3 | 87.3 |
| C9 |  |
244.7 | 4358.0 | 696.7 |
| C10 |  |
2353.5 | 6757.7 | 62.8 |
| C11 |  |
208.5 | 1934.4 | 254.6 |
| C12 |  |
52.2 | 765.7 | 19.7 |
| C13 |  |
216.9 | 1583.1 | 508.6 |
| C14 |  |
234.4 | 1420.8 | 28.1 |
| C15 |  |
16.6 | 406.2 | 31.1 |
| C16 |  |
20.5 | 1103.5 | 161.4 |
| C17 |  |
72.7 | 1831.4 | 347.8 |
| C18 |  |
339.0 | 5073.1 | 178.4 |
| C19 |  |
1649.1 | 7616.3 | 167.3 |
| C20 |  |
1103.5 | 7478.2 | 399.5 |
| C21 |  |
107.5 | 2671.4 | 54.2 |
| C22 |  |
195.8 | 1729.0 | 62.8 |
| C23 |  |
372.6 | 2748.4 | 73.3 |
| C24 |  |
127.6 | 2933.7 | 37.0 |
| C25 |  |
74.1 | 6100.4 | 193.7 |
| C26 |  |
104.6 | 906.7 | 24.7 |
| C27 |  |
138.8 | 2798.5 | 37.3 |
| C28 |  |
117.6 | 3541.8 | 563.7 |
| C29 |  |
307.5 | 9154.3 | 2040.9 |
| C30 |  |
675.8 | 4898.2 | 361.0 |
| C31 |  |
206.8 | 3608.5 | 85.9 |
| C32 |  |
255.3 | 3377.2 | 186.4 |
| C33 |  |
397.9 | 3754.0 | 41.7 |
| C34 |  |
63.6 | 70.4 | 63.1 |
| C35 |  |
36.1 | 135.8 | 184.2 |
| C36 |  |
25.8 | 226.8 | 867.9 |
| C37 |  |
79.6 | 475.7 | 974.5 |
| C38 |  |
194.0 | 457.3 | 323.7 |
| C39 |  |
472.2 | >10,000 | 221.9 |
| C40 |  |
68.1 | 1258.7 | 156.5 |
| C41 |  |
51.7 | 1565.8 | 12.2 |