| Literature DB >> 22672799 |
Daniel P Sutherlin1, Stewart Baker, Angelina Bisconte, Paul M Blaney, Anthony Brown, Bryan K Chan, David Chantry, Georgette Castanedo, Paul DePledge, Paul Goldsmith, David M Goldstein, Timothy Hancox, Jasmit Kaur, David Knowles, Rama Kondru, John Lesnick, Matthew C Lucas, Cristina Lewis, Jeremy Murray, Alan J Nadin, Jim Nonomiya, Jodie Pang, Neil Pegg, Steve Price, Karin Reif, Brian S Safina, Laurent Salphati, Steven Staben, Eileen M Seward, Stephen Shuttleworth, Sukhjit Sohal, Zachary K Sweeney, Mark Ultsch, Bohdan Waszkowycz, Binqing Wei.
Abstract
A potent inhibitor of PI3Kδ that is ≥ 200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis for selectivity is illustrated through structure activity relationships and crystal structures of compounds bound to a K802T mutant of PI3Kγ. Pharmacokinetic data in rats and mice support the use of 3 as a useful tool compound to use for in vivo studies.Entities:
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Year: 2012 PMID： 22672799 DOI： 10.1016/j.bmcl.2012.05.027
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823