期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 14, 页码 4045-4049出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.05.096
关键词
CHK1; Kinase inhibitors; Imidazopyrazines
资金
- Cancer Research UK [CUK] [C309/A2187, C309/A8274, C309/A8365]
- The Institute of Cancer Research
- NIHR Biomedical Research Centre
A range of 3,6-di(hetero)arylimidazo[1,2-a]pyrazine ATP-competitive inhibitors of CHK1 were developed by scaffold hopping from a weakly active screening hit. Efficient synthetic routes for parallel synthesis were developed to prepare analogues with improved potency and ligand efficiency against CHK1. Kinase pro. ling showed that the imidazo[1,2-a]pyrazines could inhibit other kinases, including CHK2 and ABL, with equivalent or better potency depending on the pendant substitution. These 3,6-di(hetero) aryl imidazo[1,2-a] pyrazines appear to represent a general kinase inhibitor scaffold. (C) 2010 Elsevier Ltd. All rights reserved.
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