期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 15, 页码 7347-7357出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.06.017
关键词
protein tyrosine kinases (PTKs); Syk; ZAP-70; Syk and/or ZAP-70 kinase inhibitor
Splenic tyrosine kinase (Syk) family kinases, which are members of the protein tyrosine kinase family, play crucial roles in immune responses, with Syk participating in B-cell activation and the zeta-associated protein 70 kDa (ZAP-70) kinase being involved in T-cell activation. Therefore, Syk family kinase inhibitors are candidate therapeutic agents for the treatment of various allergic disorders and autoimmune diseases. We designed 1,2,4-triazolo[4,3-c] pyrimidine and 1,2,4-triazolo[1,5-c] pyrimidine derivatives as Syk family kinase inhibitors, based on literature reports and structure-based drug design. These derivatives showed significant Syk inhibitory activities, with ZAP-70 inhibition. Representative compounds 10d and 11 not only exhibited strong inhibition of both Syk and ZAP-70 kinase but also suppressed IL-2 production by peripheral blood mononuclear cells and whole blood. (C) 2008 Elsevier Ltd. All rights reserved.
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