Abstract
A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a (125)I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using human peripheral blood mononuclear cells.
MeSH terms
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Animals
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Cell Culture Techniques
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Cell Movement / drug effects*
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Cell Movement / physiology
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Humans
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Intercellular Signaling Peptides and Proteins / metabolism
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Iodine Radioisotopes
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Leukocytes, Mononuclear / cytology
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Leukocytes, Mononuclear / metabolism
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Mice
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Models, Chemical
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Oligopeptides / metabolism
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Quinazolinones / chemical synthesis
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Quinazolinones / pharmacology*
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Radioligand Assay
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Receptors, CXCR3
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Receptors, Chemokine / antagonists & inhibitors*
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Receptors, Cytokine / metabolism
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Structure-Activity Relationship
Substances
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CXCR3 protein, human
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Cxcr3 protein, mouse
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IP10-Mig receptor
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ITAC peptide
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Intercellular Signaling Peptides and Proteins
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Iodine Radioisotopes
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Oligopeptides
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Quinazolinones
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Receptors, CXCR3
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Receptors, Chemokine
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Receptors, Cytokine