期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 5, 页码 1228-1231出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.01.005
关键词
CCR1; Chemokines; Chemokine receptor antagonists; Pyrazoles; Rheumatoid arthritis; Multiple myeloma
A novel series of CCR1 antagonists based on the 1-(4-phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanone scaffold was identified by screening a compound library utilizing CCR1-expressing human THP-1 cells. SAR studies led to the discovery of the highly potent and selective CCR1 antagonist 14 (CCR1 binding IC50 = 4 nM using [I-125]-CCL3 as the chemokine ligand). Compound 14 displayed promising pharmacokinetic and toxicological profiles in preclinical species. (c) 2013 Elsevier Ltd. All rights reserved.
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