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

  • Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. doi: 10.1016/j.bmcl.2007.03.106.
Michael Johnson  1 ,  An-Rong Li ,  Jiwen Liu ,  Zice Fu ,  Liusheng Zhu ,  Shichang Miao ,  Xuemei Wang ,  Qingge Xu ,  Alan Huang ,  Andrew Marcus ,  Feng Xu ,  Karen Ebsworth ,  Emmanuel Sablan ,  Jay Danao ,  Jeff Kumer ,  Dan Dairaghi ,  Chris Lawrence ,  Tim Sullivan ,  George Tonn ,  Thomas Schall ,  Tassie Collins ,  Julio Medina
Affiliations
  • 1. Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
PMID: 17448658 DOI: 10.1016/j.bmcl.2007.03.106
Abstract

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.

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