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

Stefania Storelli; Pauline Verdijk; Dennis Verzijl; Henk Timmerman; Andrea C van de Stolpe; Cornelis P Tensen; Martine J Smit; Iwan J P De Esch; Rob Leurs

doi:10.1016/j.bmcl.2005.03.070

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

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2910-3. doi: 10.1016/j.bmcl.2005.03.070.

Authors

Stefania Storelli¹, Pauline Verdijk, Dennis Verzijl, Henk Timmerman, Andrea C van de Stolpe, Cornelis P Tensen, Martine J Smit, Iwan J P De Esch, Rob Leurs

Affiliation

¹ Leiden/Amsterdam Center for Drug Research (LACDR), Division of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit Amsterdam, The Netherlands.

PMID: 15911279
DOI: 10.1016/j.bmcl.2005.03.070

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Humans
Quinazolines / chemical synthesis*
Quinazolines / chemistry
Quinazolines / pharmacology*
Receptors, CXCR3
Receptors, Chemokine / antagonists & inhibitors*
Spectrometry, Fluorescence
Structure-Activity Relationship

Substances

3-phenyl-3H-quinazolin-4-one
CXCR3 protein, human
Quinazolines
Receptors, CXCR3
Receptors, Chemokine