Ontology highlight
ABSTRACT:
SUBMITTER: Hoegenauer K
PROVIDER: S-EPMC4983741 | biostudies-other | 2016 Aug
REPOSITORIES: biostudies-other
ACS medicinal chemistry letters 20160602 8
Inhibition of the lipid kinase PI3Kδ is a promising principle to treat B and T cell driven inflammatory diseases. Using a scaffold deconstruction-reconstruction strategy, we identified 4-aryl quinazolines that were optimized into potent PI3Kδ isoform selective analogues with good pharmacokinetic properties. With compound 11, we illustrate that biochemical PI3Kδ inhibition translates into modulation of isoform-dependent immune cell function (human, rat, and mouse). After oral administration of co ...[more]