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

…, A Marcus, F Xu, K Ebsworth, E Sablan, J Danao…

Index: Johnson, Michael; Li, An-Rong; Liu, Jiwen; Fu, Zice; Zhu, Liusheng; Miao, Shichang; Wang, Xuemei; Xu, Qingge; Huang, Alan; Marcus, Andrew; Xu, Feng; Ebsworth, Karen; Sablan, Emmanuel; Danao, Jay; Kumer, Jeff; Dairaghi, Dan; Lawrence, Chris; Sullivan, Tim; Tonn, George; Schall, Thomas; Collins, Tassie; Medina, Julio Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 12 p. 3339 - 3343

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Citation Number: 71

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 125I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using human peripheral blood mononuclear cells.