| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372031 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Derivatives of the 4-fluorobenzyl dimethylpiperazine-indole class of p38α MAP kinase inhibitors are described. Biological evaluation of these compounds focused on maintaining activity while improving pharmacokinetic (PK) properties. Improved properties were observed for structures bearing substitutions on the benzylic methylene.
Graphical abstractSAR studies of the p38α MAP kinase inhibitor SCIO-469 focused on maintaining activity while improving pharmacokinetic properties. Advantages were noted for compounds bearing substituents on the benzylic methylene carbon.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Xuefei Tan, Richland W. Tester, Gregory R. Luedtke, Sarvajit Chakravarty, Babu J. Mavunkel, John J. Perumattam, Qing Lu, Imad Nashashibi, Joon Jung, Jie Hu, Albert Liclican, Ramona Almirez, Jocelyn Tabora, Vinh Tran, Maureen Laney, Daniel E. Levy,