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. 2019 Oct 17;10(11):1554–1560. doi: 10.1021/acsmedchemlett.9b00334

Table 2. SAR of Lactam Pyrazolopyrimidines 18–21.

graphic file with name ml9b00334_0008.jpg

Cmpda * R R′ PI3Kδ SPA IC50 (nM) SU-DHL-6 Viability IC50 (nM) Pfeiffer Proliferation IC50 (nM) Pfeiffer PBadj IC50 (nM) % fu in human plasma IntCL (L/h/kg) Caco2 Pm (×10–6 cm/s)
18   Me Me 2.4 13 51 480 10 0.7 2.8
19   Me Et 1.4 2.1 4.8 47 6.5 0.7 1.9
20 R F Et <1.0 1.6 2.5 4.2 5.8 0.7 1.0
21   CN Et <1.0 0.47 1.7 4.1 23 0.7 0.3
a

Single isomers. fu = fraction unbound.