期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 8, 页码 1336-1341出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.03.018
关键词
Dual CK2 and PIM kinase inhibitors; Cancer; 2,6-Disubstituted pyrazine
The design and synthesis of a novel series of 2,6-disubstituted pyrazine derivatives as CK2 kinase inhibitors is described. Structure-guided optimization of a 5-substituted-3-thiophene carboxylic acid screening hit (3a) led to the development of a lead compound (12b), which shows inhibition in both enzymatic and cellular assays. Subsequent design and hybridization efforts also led to the unexpected identification of analogs with potent PIM kinase activity (14f). (C) 2018 Elsevier Ltd. All rights reserved.
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