title: Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists.
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.
authors.affiliation: Leiden/Amsterdam Center for Drug Research (LACDR), Division of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit Amsterdam, The Netherlands.
authors.forename: Stefania
authors.initials: S
authors.lastname: Storelli
authors.forename: Pauline
authors.initials: P
authors.lastname: Verdijk
authors.forename: Dennis
authors.initials: D
authors.lastname: Verzijl
authors.forename: Henk
authors.initials: H
authors.lastname: Timmerman
authors.forename: Andrea C
authors.initials: AC
authors.lastname: van de Stolpe
authors.forename: Cornelis P
authors.initials: CP
authors.lastname: Tensen
authors.forename: Martine J
authors.initials: MJ
authors.lastname: Smit
authors.forename: Iwan J P
authors.initials: IJ
authors.lastname: De Esch
authors.forename: Rob
authors.initials: R
authors.lastname: Leurs
mesh_terms: D006801:Humans; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D054367:Receptors, CXCR3; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D013050:Spectrometry, Fluorescence; D013329:Structure-Activity Relationship
chemical_list: C504934:3-phenyl-3H-quinazolin-4-one; C515187:CXCR3 protein, human; D011799:Quinazolines; D054367:Receptors, CXCR3; D019707:Receptors, Chemokine