期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 21, 页码 6366-6369出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.105
关键词
Pim-kinase inhibitors; Indole; Kinase selectivity; Oncology
A series of novel 3,5-disubstituted indole derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High throughput screen identified a pan-Pim kinase inhibitor with a promiscuous scaffold. Guided by structure-based drug design, SAR of the series afforded a highly selective indole chemotype that was further developed into a potent set of compounds against Pim-1, 2, and 3 (Pim-1 and Pim-3: IC(50) <= 2 nM and Pim-2: IC(50) <= 100 nM). (C) 2011 Elsevier Ltd. All rights reserved.
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