Synthesis and SAR study of potent and selective PI3Kδ inhibitors

DOI: 10.1016/j.bmcl.2015.01.001

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1104 - 1109 (2015)

Update date:2022-07-30

Topics:

Authors:

Bui, Minna

Hao, Xiaolin

Shin, Youngsook

Cardozo, Mario

He, Xiao

Henne, Kirk

Suchomel, Julia

McCarter, John

McGee, Lawrence R.

San Miguel, Tisha

Medina, Julio C.

Mohn, Deanna

Tran, Thuy

Wannberg, Sharon

Wong, Jamie

Wong, Simon

Zalameda, Leeanne

Metz, Daniela

Cushing, Timothy D.

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Article abstract of DOI:10.1016/j.bmcl.2015.01.001

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.

Full text of DOI:10.1016/j.bmcl.2015.01.001

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Product name:2-ethyl-6-fluoro-3-(pyridin-2-yl)quinoline-4-carboxamide

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