Synthesis and structure–activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists

S Storelli, P Verdijk, D Verzijl, H Timmerman…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 11 p. 2910 - 2913

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Citation Number: 31

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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