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. 2016 Oct 28;7(12):1161–1166. doi: 10.1021/acsmedchemlett.6b00356

Table 2. C-3 Pyrazolopyrimidine Modifications to Give Compounds 1421.

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
a

IC50 not determined; inhibition of BTK was 66% at 100 nM 14.

b

IC50 not determined; inhibition of PI3Kδ was 41% at 100 nM 14.