Table 2.
SAR exploration of the R1/R3 positions.
| |||||
|---|---|---|---|---|---|
| Compd. | R1 | R3 | Tel-c-KIT-BaF3 (GI50: μM) |
Parental BaF3 (GI50: μM) |
K562 (GI50: μM) |
| 6n |
|
|
0.031 | 6.39 | 2.32 |
| 6o |
|
|
0.083 | 5.47 | 5.85 |
| 6p |
|
|
0.10 | >10 | 5.24 |
| 6q |
|
|
0.065 | 8.94 | 1.96 |
| 6r |
|
|
0.16 | >10 | 3.66 |
| 6s |
|
|
0.15 | >10 | 1.95 |
| 6t |
|
|
0.15 | >10 | 4.56 |
| 6u |
|
|
>10 | >10 | >10 |
| 6v |
|
|
>10 | >10 | >10 |
| 10a |
|
|
1.48 | >10 | >10 |
| 10b |
|
|
0.34 | >10 | 9.92 |
| 10c |
|
|
4.8 | >10 | >10 |
| 10d |
|
|
5.55 | >10 | >10 |
| 13 |
|
|
2.6 | 3.3 | 0.78 |