Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 15, Pages 4715-4718Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.024
Keywords
MAPKAP-K2; MK2; TNFa; Inhibition; Antiinflammatory; In vivo; Rheumatoid arthritis
Categories
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available