Abstract
2,3,4-Substituted quinolines such as (10a) were found to be potent inhibitors of PI3Kδ in both biochemical and cellular assays with good selectivity over three other class I PI3K isoforms. Some of those analogs showed favorable pharmacokinetic properties.
Keywords:
Autoimmune disorders; Inflammation; PI3Kδ; Reversed quinolines.
Copyright © 2015 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Class I Phosphatidylinositol 3-Kinases / antagonists & inhibitors*
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Class I Phosphatidylinositol 3-Kinases / metabolism
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Humans
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Male
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Protein Isoforms / antagonists & inhibitors
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Protein Isoforms / metabolism
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacokinetics
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Protein Kinase Inhibitors / pharmacology*
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Quinolines / chemical synthesis
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Quinolines / chemistry*
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Quinolines / pharmacokinetics
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Quinolines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
Substances
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Protein Isoforms
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Protein Kinase Inhibitors
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Quinolines
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Class I Phosphatidylinositol 3-Kinases