期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 2, 页码 619-623出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.11.074
关键词
CK2; kinase; anticancer
A series of macrocyclic derivatives has been designed and synthesized based on the X-ray co-crystal structures of pyrazolo[1,5-a] [1,3,5]triazines with corn CK2 (cCK2) protein. Bioassays demonstrated that these macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds are potent CK2 inhibitors with K-i around 1.0 nM and strongly inhibit cancer cell growth with IC50 as low as similar to 100 nM. (c) 2007 Elsevier Ltd. All rights reserved.
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