Table 2. Kinase-Inhibitory and Antiproliferative Activities of Pyrazolo[1,5-a]pyrimidine Derivatives.
| IC50 (μM)a |
GI50 (μM)a |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| FLT3-ITD | FLT3-D835Y | CDK2/E | MV4-11 | MOLM-13 | SEM | CEM | NOMO-1 | ML-2 | K562 | |
| 9 | >20 | NT | >20 | 7.360 | 3.285 | 1.575 | 3.595 | >10 | >10 | >10 |
| 10a | 10.612 | NT | >20 | >10 | >10 | >10 | >10 | >10 | >10 | >10 |
| 10b | 2.507 | NT | >20 | 5.737 | 3.280 | 9.840 | >10 | >10 | >10 | >10 |
| 11 | 0.540 | 0.109 | 0.774 | 1.817 | 2.553 | 5.510 | >10 | >10 | >10 | >10 |
| 14 | 0.623 | 0.272 | 0.100 | 0.690 | 1.413 | 7.905 | >10 | >10 | >10 | >10 |
a
For SD values, see Table S3 in the Supporting Information. NT = not tested.