Discovery of Orally Efficacious Phosphoinositide 3‑Kinase δ Inhibitors with Improved Metabolic Stability
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https://figshare.com/articles/dataset/Discovery_of_Orally_Efficacious_Phosphoinositide_3_Kinase_Inhibitors_with_Improved_Metabolic_Stability/3979158
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资源简介：
Aberrant signaling of phosphoinositide
3-kinase δ (PI3Kδ)
has been implicated in numerous pathologies including hematological
malignancies and rheumatoid arthritis. Described in this manuscript
are the discovery, optimization, and in vivo evaluation of a novel
series of pyridine-containing PI3Kδ inhibitors. This work led
to the discovery of 35, a highly selective inhibitor
of PI3Kδ which displays an excellent pharmacokinetic profile
and is efficacious in a rodent model of rheumatoid arthritis.
创建时间：
2016-10-07
