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

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.
Stefania Storelli 1,  Pauline Verdijk,  Dennis Verzijl,  Henk Timmerman,  Andrea C van de Stolpe,  Cornelis P Tensen,  Martine J Smit,  Iwan J P De Esch,  Rob Leurs
Affiliations

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.

Figures