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一系列喹唑啉酮衍生的CXCR3拮抗剂的发现与优化

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

作者信息

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

机构信息

Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.

出版信息

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. doi: 10.1016/j.bmcl.2007.03.106. Epub 2007 Apr 6.

DOI:10.1016/j.bmcl.2007.03.106
PMID:17448658
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.

摘要

已经合成了一系列喹唑啉酮衍生的CXCR3受体抑制剂,并评估了它们对该受体的亲和力。使用人外周血单核细胞,通过(125)I-IP10置换试验以及针对IP10、ITAC和MIG的体外细胞迁移试验对化合物进行了评估。

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