| Literature DB >> 17055721 |
Charles L Cywin1, Georg Dahmann, Anthony S Prokopowicz, Erick R R Young, Ronald L Magolda, Mario G Cardozo, Derek A Cogan, Darren Disalvo, John D Ginn, Mohammed A Kashem, John P Wolak, Carol A Homon, Thomas M Farrell, Heather Grbic, Hanbo Hu, Paul V Kaplita, Lisa H Liu, Denice M Spero, Deborah D Jeanfavre, Kathy M O'Shea, Della M White, Joseph R Woska, Maryanne L Brown.
Abstract
An uHTS campaign was performed to identify selective inhibitors of PKC-theta. Initial triaging of the hit set based on selectivity and historical analysis led to the identification of 2,4-diamino-5-nitropyrimidines as potent and selective PKC-theta inhibitors. A homology model and initial SAR is presented demonstrating that a 2-arylalkylamino substituent in conjunction with suitable 4-diamino substituent are essential for achieving selectivity over many kinases. Additional hit to lead profiling is presented on selected compounds.Entities:
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Year: 2006 PMID： 17055721 DOI： 10.1016/j.bmcl.2006.09.056
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823