Design and synthesis of phenethyl benzo [1, 4] oxazine-3-ones as potent inhibitors of PI3Kinaseγ

…, M Visnick, JL Mobley, DT Dudley, TJ Baginski…

Index: Lanni Jr., Thomas B.; Greene, Keri L.; Kolz, Christine N.; Para, Kimberly S.; Visnick, Melean; Mobley, James L.; Dudley, David T.; Baginski, Theodore J.; Liimatta, Marya B. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 3 p. 756 - 760

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Citation Number: 43

Abstract

The Type 1 PI3Kinases comprise a family of enzymes, which primarily phosphorylate PIP2 to give the second messenger PIP3, a key player in many intracellular signaling processes [Science, 2002, 296, 1655; Trends Pharmacol. Sci. 2003, 24, 366]. Of the four type 1 PI3Ks, the γ-isoform, which is expressed almost exclusively in leukocytes [Curr. Biol., 1997, 7, R470], is of particular interest with respect to its role in inflammatory diseases such as ...