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. 2015 Jul 23;58(14):5684-8.
doi: 10.1021/acs.jmedchem.5b00498. Epub 2015 Jul 6.

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ

Philip N Collier  1 , David Messersmith  1 , Arnaud Le Tiran  1 , Upul K Bandarage  1 , Christina Boucher  1 , Jon Come  1 , Kevin M Cottrell  1 , Veronique Damagnez  1 , John D Doran  1 , James P Griffith  1 , Suvarna Khare-Pandit  1 , Elaine B Krueger  1 , Mark W Ledeboer  1 , Brian Ledford  1 , Yusheng Liao  1 , Sudipta Mahajan  1 , Cameron S Moody  1 , Setu Roday  1 , Tiansheng Wang  1 , Jinwang Xu  1 , Alex M Aronov  1
Affiliations

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ

Philip N Collier et al. J Med Chem. .

Abstract

A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase structure. Optimization of the alkylimidazole group led to inhibitors with higher levels of PI3Kγ selectivity. Additional insights into PI3K isoform selectivity related to sequence differences in a known distal hydrophobic pocket are also described.

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