Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 13, Pages 4296-4302Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.05.027
Keywords
PI3K delta inhibitor; PI3K Isoform selectivity; B-cell inhibition; Rhumatoid arthritis
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A potent inhibitor of PI3K delta that is >= 200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis for selectivity is illustrated through structure activity relationships and crystal structures of compounds bound to a K802T mutant of PI3K gamma. Pharmacokinetic data in rats and mice support the use of 3 as a useful tool compound to use for in vivo studies. (C) 2012 Elsevier Ltd. All rights reserved.
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