Table 3.
Investigation of sulphonamide and ether derivatives.
| ||||||
|---|---|---|---|---|---|---|
| Name | R1 | X1 | X2 | TLK2 IC50(nM)a | FLT3 (%)b | TRKC (%)b |
| 52 |
|
C-H | C-H | > 20000 | 31 | 1.6 |
| 53 | N | C-H | > 20000 | 55 | 12 | |
| 54 |
|
C-H | C-H | > 20000 | 27 | 3.0 |
| 55 | N | C-H | > 20000 | 62 | 27 | |
| 57 |
|
C-H | C-H | 560 | 8.3 | 2.8 |
| 58 | N | C-H | 1600 | 33 | 11 | |
| 59 | C-H | N | 160 | 25 | 5.9 | |
8-point dose response (n=1);
percentage inhibition at 0.5 μM (n=2)