Table 18.
Inhibitory activities of compounds 122j–n, 130a–m, and 127a–y against kinases.
| Compd. | R2 | IC50 (nM) | Compd. | R2 | IC50 (nM) | ||||
|---|---|---|---|---|---|---|---|---|---|
| c-KIT | PDGFRα | VEGFR2 | c-KIT | PDGFRα | VEGFR2 | ||||
| 122j |
|
10,890 | 305 | 4322 | 127e |
|
1.4 | 27 | 10,462 |
| 122k |
|
1831 | 65 | 5613 | 127f |
|
320 | 1123 | 8634 |
| 122l |
|
4794 | 262 | 6228 | 127g |
|
1416 | 1465 | 11,382 |
| 122m |
|
2402 | 182 | 4050 | 127h |
|
553 | 1133 | 4523 |
| 122n |
|
201 | 21,400 | >50,000 | 127i |
|
318 | 732 | 5002 |
| 130a |
|
19 | 215 | 6235 | 127j |
|
144 | 576 | 6229 |
| 130b |
|
1949 | 1779 | 3940 | 127k |
|
>50,000 | >50,000 | >50,000 |
| 130c |
|
7.2 | 127 | 3695 | 127l |
|
51 | 387 | 3503 |
| 130d |
|
2.4 | 7.2 | 2280 | 127m |
|
26 | 157 | 1791 |
| 130e |
|
2225 | 1101 | 6816 | 127n |
|
78 | 472 | 4079 |
| 130f |
|
4581 | 928 | 4164 | 127o |
|
46,064 | >50,000 | >50,000 |
| 130g |
|
397 | 18,925 | 26,163 | 127p |
|
3.7 | 82 | 9760 |
| 130h |
|
6438 | 4077 | 36,890 | 127q |
|
1.7 | 24 | 3857 |
| 130i |
|
12 | 136 | 41,966 | 127r |
|
6.2 | 135 | 10,917 |
| 130j |
|
12 | 176 | 5352 | 127s |
|
8.7 | 83 | >50,000 |
| 130k |
|
2.6 | 83 | 6920 | 127t |
|
120 | 411 | 2391 |
| 130l |
|
9.3 | 309 | 9046 | 127u |
|
20 | 401 | >50,000 |
| 130m |
|
22,056 | 4608 | 15,935 | 127v |
|
14 | 313 | 3109 |
| 127a |
|
38,667 | >50,000 | >50,000 | 127w |
|
1.9 | 22 | 1845 |
| 127b |
|
21,432 | >50,000 | >50,000 | 127x |
|
20 | 124 | >50,000 |
| 127c |
|
20,556 | 43,877 | >50,000 | 127y |
|
3.6 | 97 | >50,000 |
| 127d |
|
3.5 | 164 | >50,000 | |||||