期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 1, 页码 471-474出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.10.114
关键词
Kinase; CHK1; Pyrazolo[1,5-a]pyrimidine; CDK; Cell cycle; Inhibitors
Previous efforts by our group have established pyrazolo[1,5-a]pyrimidine as a viable core for the development of potent and selective CDK inhibitors. As part of an effort to utilize the pyrazolo[1,5-a]pyrimidine core as a template for the design and synthesis of potent and selective kinase inhibitors, we focused on a key regulator in the cell cycle progression, CHK1. Continued SAR development of the pyrazolo [1,5-a]pyrimidine core at the C5 and C6 positions, in conjunction with previously disclosed SAR at the C3 and C7 positions, led to the discovery of potent and selective CHK1 inhibitors. (c) 2010 Elsevier Ltd. All rights reserved.
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