期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 15, 页码 4715-4718出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.024
关键词
MAPKAP-K2; MK2; TNFa; Inhibition; Antiinflammatory; In vivo; Rheumatoid arthritis
Pyrrolo[2,3-f]isoquinoline based amino acids, tetracyclic lactams and cyclic ketone analogues are described as novel MK2 inhibitors with IC(50) as low as 5 nM and good selectivity profiles against a number of related kinases including ERK, p38 alpha and JNKs. TNF alpha release was suppressed from human peripheral blood mononuclear cells (hPBMCs), and a representative compound inhibited LPS induced TNF alpha release in mice illustrating the potential of this series to provide orally active MK2 inhibitors. (C) 2010 Elsevier Ltd. All rights reserved.
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