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- W2560024871 abstract "The delta isoform of the phosphatidylinositol 3-kinase (PI3Kδ) has been shown to have an essential role in specific immune cell functions and thus represents a potential therapeutic target for autoimmune and inflammatory diseases. Herein, the optimization of a series of pyrrolotriazinones as potent and selective PI3Kδ inhibitors is described. The main challenge of the optimization process was to identify an orally available compound with a good pharmacokinetic profile in preclinical species that predicted a suitable dosing regimen in humans. Structure–activity relationships and structure–property relationships are discussed. This medicinal chemistry exercise led to the identification of LAS191954 as a candidate for clinical development." @default.
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- W2560024871 date "2016-12-07" @default.
- W2560024871 modified "2023-10-18" @default.
- W2560024871 title "Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases" @default.
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- W2560024871 doi "https://doi.org/10.1021/acsmedchemlett.6b00438" @default.
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