Evolution of a novel orally bioavailable series of PI3Kδ inhibitors from an inhaled lead for the treatment of respiratory disease.

Augustin Amour, Nick Barton, Anthony W.J. Cooper, Graham Inglis, Craig Jamieson, Christopher N. Luscombe, David Perez, Simon Peace, Paul Rowland, Chris Tame, Sorif Uddin, Giovanni Vitulli, Natalie Wellaway

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

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.
LanguageEnglish
Number of pages34
JournalJournal of Medicinal Chemistry
Early online date18 Jul 2016
DOIs
Publication statusE-pub ahead of print - 18 Jul 2016

Fingerprint

Phosphatidylinositol 3-Kinases
Growth
Lead

Keywords

  • PI3Kδ inhibitors
  • respiratory disease
  • bioavailability
  • deconstruction
  • hinge-binding groups
  • optimisation
  • indazole core
  • physicochemical properties
  • pharmacokinetic properties

Cite this

Amour, Augustin ; Barton, Nick ; Cooper, Anthony W.J. ; Inglis, Graham ; Jamieson, Craig ; Luscombe, Christopher N. ; Perez, David ; Peace, Simon ; Rowland, Paul ; Tame, Chris ; Uddin, Sorif ; Vitulli, Giovanni ; Wellaway, Natalie. / Evolution of a novel orally bioavailable series of PI3Kδ inhibitors from an inhaled lead for the treatment of respiratory disease. In: Journal of Medicinal Chemistry. 2016.
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abstract = "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.",
keywords = "PI3Kδ inhibitors, respiratory disease, bioavailability, deconstruction, hinge-binding groups, optimisation, indazole core, physicochemical properties, pharmacokinetic properties",
author = "Augustin Amour and Nick Barton and Cooper, {Anthony W.J.} and Graham Inglis and Craig Jamieson and Luscombe, {Christopher N.} and David Perez and Simon Peace and Paul Rowland and Chris Tame and Sorif Uddin and Giovanni Vitulli and Natalie Wellaway",
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Amour, A, Barton, N, Cooper, AWJ, Inglis, G, Jamieson, C, Luscombe, CN, Perez, D, Peace, S, Rowland, P, Tame, C, Uddin, S, Vitulli, G & Wellaway, N 2016, 'Evolution of a novel orally bioavailable series of PI3Kδ inhibitors from an inhaled lead for the treatment of respiratory disease.' Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.6b00799

Evolution of a novel orally bioavailable series of PI3Kδ inhibitors from an inhaled lead for the treatment of respiratory disease. / Amour, Augustin; Barton, Nick; Cooper, Anthony W.J.; Inglis, Graham; Jamieson, Craig; Luscombe, Christopher N.; Perez, David; Peace, Simon; Rowland, Paul; Tame, Chris; Uddin, Sorif; Vitulli, Giovanni; Wellaway, Natalie.

In: Journal of Medicinal Chemistry, 18.07.2016.

Research output: Contribution to journalArticle

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AU - Jamieson, Craig

AU - Luscombe, Christopher N.

AU - Perez, David

AU - Peace, Simon

AU - Rowland, Paul

AU - Tame, Chris

AU - Uddin, Sorif

AU - Vitulli, Giovanni

AU - Wellaway, Natalie

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KW - hinge-binding groups

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