期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 16, 页码 4758-4761出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.06.065
关键词
Tpl2 kinase; Indazole; Rheumatoid arthritis
Synthesis, modeling and structure-activity relationship of indazoles as inhibitors of Tpl2 kinase are described. From a high throughput screening effort, we identified an indazole hit compound 5 that has a single digit micromolar Tpl2 activity. Through SAR modifications at the C3 and C5 positions of the indazole, we discovered compound 31 with good potency in LANCE assay and cell-based p-Erk assay. (C) 2011 Elsevier Ltd. All rights reserved.
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