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

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

Bioorganic & medicinal chemistry letters (2007-04-24)
Michael Johnson, 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
PMID17448658
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.