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Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors.

Abstract：

:In this paper, we describe the discovery and optimization of a new chemotype of isoform selective PI3Kγ inhibitors. Starting from an HTS hit, potency and physicochemical properties could be improved to give compounds such as 15, which is a potent and remarkably selective PI3Kγ inhibitor with ADME properties suitable for oral administration. Compound 15 was advanced into in vivo studies showing dose-dependent inhibition of LPS-induced airway neutrophilia in rats when administered orally.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Pemberton N,Mogemark M,Arlbrandt S,Bold P,Cox RJ,Gardelli C,Holden NS,Karabelas K,Karlsson J,Lever S,Li X,Lindmark H,Norberg M,Perry MWD,Petersen J,Rodrigo Blomqvist S,Thomas M,Tyrchan C,Westin Eriksson A,Zlatoidsky

doi

10.1021/acs.jmedchem.8b00447

subject

Has Abstract

pub_date

2018-06-28 00:00:00

pages

5435-5441

issue

12

eissn

0022-2623

issn

1520-4804

journal_volume

61

pub_type

杂志文章

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