Table 2. SAR exploration of the linker and substituents in the head group.
| ||||
|---|---|---|---|---|
| Cpd. | R1 | Linker | R2 | AXL IC50 (nM) |
| w5 |
|
|
Methyl- | 20 |
| w6 |
|
|
|
30 |
| w7 |
|
|
|
8 |
| w8 |
|
|
|
5 |
| w9 |
|
|
|
17 |
| w10 |
|
|
|
4 |
| w11 |
|
|
Methyl- | 5 |
| w12 |
|
|
Methyl- | 5 |
| w13 |
|
|
Methyl- | 24 |
| w14 |
|
|
|
6 |
| w15 |
|
|
|
8 |
| w16 |
|
|
|
11 |
| w17 |
|
|
|
10 |
| w18 |
|
|
Methyl- | 5 |
| w19 |
|
|
Methyl- | 16 |
| w20 |
|
|
Methyl- | 51 |
| w21 |
|
|
Methyl- | 35 |
| w22 |
|
|
Methyl- | 18 |
| w23 |
|
|
Methyl- | 12 |
| w24 |
|
|
|
6 |
| w25 |
|
|
|
15 |