Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists.
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.
Storelli
Stefania
S
Leiden/Amsterdam Center for Drug Research (LACDR), Division of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit Amsterdam, The Netherlands.
Verdijk
Pauline
P
Verzijl
Dennis
D
Timmerman
Henk
H
van de Stolpe
Andrea C
AC
Tensen
Cornelis P
CP
Smit
Martine J
MJ
De Esch
Iwan J P
IJ
Leurs
Rob
R
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
C504934:3-phenyl-3H-quinazolin-4-one; C515187:CXCR3 protein, human; D011799:Quinazolines; D054367:Receptors, CXCR3; D019707:Receptors, Chemokine