Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease

Autor:	Sorif Uddin, Graham G. A. Inglis, Paul Rowland, Christopher J. Tame, Christopher N. Luscombe, Nick Barton, Natalie Wellaway, Anthony William James Cooper, Josie Morrell, Giovanni Vitulli, David Perez, Augustin Amour, Simon Peace, Craig Jamieson
Rok vydání:	2016
Předmět:	Male Models Molecular 0301 basic medicine Respiratory Tract Diseases Biological Availability Pharmacology Rats sprague dawley RS Rats Sprague-Dawley Structure-Activity Relationship 03 medical and health sciences In vivo Administration Inhalation Drug Discovery medicine Animals Protein Kinase Inhibitors Phosphoinositide-3 Kinase Inhibitors Dose-Response Relationship Drug Molecular Structure Chemistry Respiratory disease medicine.disease Rats Bioavailability Class Ia Phosphatidylinositol 3-Kinase 030104 developmental biology Molecular Medicine Biological availability
Zdroj:	Journal of Medicinal Chemistry. 59:7239-7251
ISSN:	1520-4804 0022-2623
DOI:	10.1021/acs.jmedchem.6b00799
Popis:	A four step process of high quality modelling of existing data, deconstruction, identification of replacement cores and an innovative synthetic re-growth strategy led to the rapid discovery of a novel oral series of PI3K δ inhibitors with promising selectivity and excellent in vivo characteristics.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eab7b0c93c6a62dbb34f4fe7ac3288ff https://doi.org/10.1021/acs.jmedchem.6b00799 Zobrazit plný text záznamu