944915-75-7Relevant academic research and scientific papers
Optimization of a series of quinazolinone-derived antagonists of CXCR3
Liu, Jiwen,Fu, Zice,Li, An-Rong,Johnson, Michael,Zhu, Liusheng,Marcus, Andrew,Danao, Jay,Sullivan, Tim,Tonn, George,Collins, Tassie,Medina, Julio
scheme or table, p. 5114 - 5118 (2010/03/31)
The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led to the discovery of compounds devoi
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3
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
, p. 3339 - 3343 (2008/02/11)
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, IT
