Table 2. C-3 Pyrazolopyrimidine Modifications to Give Compounds 14–21.
No. | Ar | BTK (IC50, nM) | PI3Kδ (IC50, nM) |
---|---|---|---|
14 | 3-OH-Ph | NDa | NDb |
15 | 3-Cl-5-OH-Ph | 142 | 4 |
16 | 4-F-5-OH-Ph | 7 | 61 |
17 | 4-Cl-5-OH-Ph | 14 | 33 |
18 | 4-Br-5-OH-Ph | 12 | 8 |
19 | 3-OH-4-Me-Ph | 43 | 172 |
20 | 3-OH-4-OMe-Ph | 84 | 32 |
21 | 3,4-diF-5-OH-Ph | 27 | 3 |
IC50 not determined; inhibition of BTK was 66% at 100 nM 14.
IC50 not determined; inhibition of PI3Kδ was 41% at 100 nM 14.