Identification and initial evaluation of 4-N-aryl-[1, 4] diazepane ureas as potent CXCR3 antagonists

…, C Haskell, S Ribeiro, KC Appell, I Henderson…

文献索引：Cole, Andrew G.; Stroke, Ilana L.; Brescia, Marc-Raleigh; Simhadri, Srilatha; Zhang, Joan J.; Hussain, Zahid; Snider, Michael; Haskell, Christopher; Ribeiro, Sofia; Appell, Kenneth C.; Henderson, Ian; Webb, Maria L. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 1 p. 200 - 203

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被引用次数: 37

摘要

The identification and evaluation of aryl-[1, 4] diazepane ureas as functional antagonists of the chemokine receptor CXCR3 are described. Specific examples exhibit IC50 values of∼ 60nM in a calcium mobilization functional assay, and dose-dependently inhibit CXCR3 functional response to CXCL11 (interferon-inducible T-cell α chemoattractant/I-TAC) as measured by T-cell chemotaxis, with a potency of approximately 100nM.