Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists |
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| Authors: | Storelli Stefania Verdijk Pauline Verzijl Dennis Timmerman Henk van de Stolpe Andrea C Tensen Cornelis P Smit Martine J De Esch Iwan J P Leurs Rob |
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| Institution: | Leiden/Amsterdam Center for Drug Research (LACDR), Division of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit Amsterdam, The Netherlands. |
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| Abstract: | A series of 3-phenyl-3H-quinazolin-4-ones have been synthesized and tested for affinity and activity at the chemokine CXCR3 receptor. The most potent compound (1d) has been evaluated using radioligand binding and calcium mobilization assays and is considered a useful tool for further characterization of the CXCR3 receptor. |
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