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. 2015 Mar 1;25(5):1104-9.
doi: 10.1016/j.bmcl.2015.01.001. Epub 2015 Jan 17.

Synthesis and SAR study of potent and selective PI3Kδ inhibitors

Minna Bui  1 , Xiaolin Hao  1 , Youngsook Shin  1 , Mario Cardozo  1 , Xiao He  1 , Kirk Henne  2 , Julia Suchomel  1 , John McCarter  3 , Lawrence R McGee  1 , Tisha San Miguel  4 , Julio C Medina  1 , Deanna Mohn  4 , Thuy Tran  2 , Sharon Wannberg  4 , Jamie Wong  2 , Simon Wong  2 , Leeanne Zalameda  4 , Daniela Metz  4 , Timothy D Cushing  1
Affiliations

Synthesis and SAR study of potent and selective PI3Kδ inhibitors

Minna Bui et al. Bioorg Med Chem Lett. .

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.

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