Synthesis and SAR study of potent and selective PI3Kδ inhibitors
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.
Graphical abstract
Keywords
PI3Kδ;
Reversed quinolines;
Inflammation;
Autoimmune disorders
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