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

Amour, Augustin and Barton, Nick and Cooper, Anthony W.J. and Inglis, Graham and Jamieson, Craig and Luscombe, Christopher N. and Perez, David and Peace, Simon and Rowland, Paul and Tame, Chris and Uddin, Sorif and Vitulli, Giovanni and Wellaway, Natalie (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. ISSN 0022-2623

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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.