4-苯胺基-7-吡啶基-3-喹啉甲腈作为Src激酶抑制剂
4-Anilino-7-pyridyl-3-quinolinecarbonitriles as Src kinase inhibitors.
作者信息
Zhang Nan, Wu Biqi, Boschelli Diane H, Golas Jennifer M, Boschelli Frank
机构信息
Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5071-4. doi: 10.1016/j.bmcl.2009.07.043. Epub 2009 Jul 10.
A series of 4-anilino-7-pyridyl-3-quinolinecarbonitriles was prepared as Src kinase inhibitors. A systematic SAR study of substitutions on both the pyridine ring and the 3-quinolinecarbonitrile core established the requirements for optimal activity. The lead compound, 17, showed potent activity in both the Src enzyme assay and cell assays, and demonstrated in vivo anti-tumor activity in a xenograft model.
制备了一系列4-苯胺基-7-吡啶基-3-喹啉甲腈作为Src激酶抑制剂。对吡啶环和3-喹啉甲腈核心上的取代基进行了系统的构效关系研究，确定了最佳活性的要求。先导化合物17在Src酶分析和细胞分析中均显示出强效活性，并在异种移植模型中表现出体内抗肿瘤活性。
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