期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 1, 页码 225-230出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.09.056
关键词
PKC-theta; kinase; inhibitor; hit to lead
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. (c) 2006 Elsevier Ltd. All rights reserved.
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