Table 4.
Initial investigation of amide derivatives.
| ||||||
|---|---|---|---|---|---|---|
| Name | R1 | X1 | X2 | TLK2IC50(nM)a | FLT3 (%)b | TRKC (%)b |
| 65 |
|
C-H | C-H | 170 | 11 | 4.9 |
| 66 |
|
C-H | C-H | 2400 | 25 | 2.3 |
| 67 | N | C-H | 2300 | 61 | 6.0 | |
| 68 | C-H | N | 2500 | 75 | 15 | |
| 69 |
|
C-H | C-H | 150 | 28 | 11 |
| 70 | N | C-H | 100 | 46 | 16 | |
| 71 | C-H | N | 130 | 58 | 32 | |
| 72 |
|
C-H | C-H | 820 | 21 | 19 |
| 73 | N | C-H | 34 | 44 | 30 | |
| 74 | C-H | N | 110 | 48 | 33 | |
| 75 |
|
C-H | C-H | 120 | 30 | 28 |
| 76 | C-H | N | 130 | 42 | 33 | |
8-point dose response (n=1);
percentage inhibition at 0.5 μM (n=2)