Table 1.
SAR exploration of the R1/R2/R4 positions.
| ||||||
|---|---|---|---|---|---|---|
| Compd. | R1 | R2 | R4 | Tel-c-KIT-BaF3 (GI50: μM) |
Parental BaF3 (GI50: μM) |
K562 (GI50: μM) |
| I |
|
|
–Me | 0.40 | >10 | 0.12 |
| 6a |
|
|
–Me | 7.94 | >10 | >10 |
| 6b |
|
|
–Me | 9.97 | >10 | >10 |
| 6c |
|
|
–Me | 0.11 | >10 | 2.94 |
| 6d |
|
|
–Me | 0.33 | >10 | >10 |
| 6e |
|
|
–Me | 0.19 | >10 | >10 |
| 6f |
|
|
–Me | 0.22 | >10 | 0.16 |
| 6g |
|
|
–Me | 1.55 | >10 | >10 |
| 6h |
|
|
–Me | 0.62 | >10 | 8.36 |
| 6i |
|
|
–H | 8.07 | 8.07 | >10 |
| 6j |
|
|
–H | >10 | >10 | >10 |
| 6k |
|
|
–H | 0.49 | >10 | >10 |
| 6l |
|
|
–Cl | 0.96 | >10 | 2.8 |
| 6m |
|
|
–OMe | >10 | >10 | >10 |