Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3

Michael Johnson,An-Rong Li,Jiwen Liu,Zice Fu,Liusheng Zhu,Shichang Miao,Xuemei Wang,Qingge Xu,Alan Huang,Andrew P. Marcus,Feng Xu,Karen Ebsworth,Emmanuel Sablan,Jay Danao,Jeff Kumer,Dan Dairaghi,Chris Lawrence,Timothy Sullivan,George Tonn,Thomas J. Schall,Tassie L. Collins,Julio C. Medina

Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3

2007

A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a 125 I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using human peripheral blood mononuclear cells.

Keywords:

In vivo
Cell migration
CXCR3
Peripheral blood mononuclear cell
Chemokine receptor
Biochemistry
Receptor
In vitro
Quinazolinone
Chemistry

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