Optimization of a series of multi-isoform PI3 kinase inhibitors

…, L Gowers, L James, K Jenkins, C Lock, V Sabin…

文献索引：Perry, Benjamin; Beevers, Rebekah; Bennett, Gavin; Buckley, George; Crabbe, Tom; Gowers, Lewis; James, Lynwen; Jenkins, Kerry; Lock, Chris; Sabin, Verity; Wright, Sara Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 19 p. 5299 - 5302

全文：HTML全文

被引用次数: 14

摘要

... Bioorganic & Medicinal Chemistry Letters. ... As shown in Figure 2a, 8g and 10d inhibited CD3-induced IL2 release in male Lewis rats with ED 50 s of 5 mg/kg and 20 mg/kg, respectively, compared with an ED 50 of 25 mg/kg for compound 1. When efficacy in vivo is represented using free compound exposure in plasma (EC 50 free) for this series, a good correlation is seen to the in vitro potency (Fig. ...