870998-13-3Relevant articles and documents
SUBSTITUTED [1,4]-DIAZEPANES AS CXCR3 ANTAGONISTS AND THEIR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS
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Page/Page column 20; 49, (2008/06/13)
CXCR3 inhibitors of formula are disclosed. Inhibition of CXCR3 activation is useful for treating disorders resulting from CXCR3 -associated T-cell mediated function, such as inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis and diabetes
Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonists
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.
, p. 200 - 203 (2007/10/03)
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 ~60 nM 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 100 nM.