期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 15, 页码 4374-4380出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.05.075
关键词
Casein kinase 1 delta/epsilon inhibitor; Selective CK1 delta/epsilon inhibitor; Purine scaffold kinase inhibitor; Antiproliferative agent; Potent growth inhibitor of A375 melanoma cell line
资金
- NIH Molecular Library Screening Center Network [U54MH074404]
- Rendina Family Foundation
- State of Florida to Scripps Florida
- Marie Mayer Fellowship
The development of a series of potent and highly selective casein kinase 1 delta/epsilon (CK1 delta/epsilon) inhibitors is described. Starting from a purine scaffold inhibitor (SR-653234) identified by high throughput screening, we developed a series of potent and highly kinase selective inhibitors, including SR-2890 and SR-3029, which have IC50 <= 50 nM versus CK1 delta. The two lead compounds have <= 100 nM EC50 values in MTT assays against the human A375 melanoma cell line and have physical, in vitro and in vivo PK properties suitable for use in proof of principle animal xenograft studies against human cancer cell lines. (C) 2013 Elsevier Ltd. All rights reserved.
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