2. Academic Validation
  3. Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease

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

  • J Med Chem. 2016 Aug 11;59(15):7239-51. doi: 10.1021/acs.jmedchem.6b00799.
Augustin Amour 1,  Nick Barton 1,  Anthony W J Cooper 1,  Graham Inglis 1,  Craig Jamieson 2,  Christopher N Luscombe 1,  Josie Morrell 1,  Simon Peace 1,  David Perez 1,  Paul Rowland 1,  Christopher J Tame 1,  Sorif Uddin 1,  Giovanni Vitulli 1,  Natalie Wellaway 1
Affiliations

Affiliations

  • 1 GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage SG1 2NY, U.K.
  • 2 Department of Pure and Applied Chemistry, University of Strathclyde , 295 Cathedral Street, Glasgow G1 1XL, U.K.
PMID: 27429068 DOI: 10.1021/acs.jmedchem.6b00799
Abstract

A four-step process of high-quality modeling of existing data, deconstruction, identification of replacement cores, and an innovative synthetic regrowth strategy led to the rapid discovery of a novel oral series of PI3Kδ inhibitors with promising selectivity and excellent in vivo characteristics.

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