| Literature DB >> 26121481 |
Philip N Collier1, David Messersmith1, Arnaud Le Tiran1, Upul K Bandarage1, Christina Boucher1, Jon Come1, Kevin M Cottrell1, Veronique Damagnez1, John D Doran1, James P Griffith1, Suvarna Khare-Pandit1, Elaine B Krueger1, Mark W Ledeboer1, Brian Ledford1, Yusheng Liao1, Sudipta Mahajan1, Cameron S Moody1, Setu Roday1, Tiansheng Wang1, Jinwang Xu1, Alex M Aronov1.
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.Entities:
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Year: 2015 PMID： 26121481 DOI： 10.1021/acs.jmedchem.5b00498
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446