4-（2-芳基-环丙基氨基）喹啉-3-腈作为表皮生长因子受体酪氨酸激酶抑制剂的合成及构效关系
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
作者信息
Pannala Madhavi, Kher Sunil, Wilson Norma, Gaudette John, Sircar Ila, Zhang Shao-Hui, Bakhirev Alexei, Yang Guang, Yuen Phoebe, Gorcsan Frank, Sakurai Naoki, Barbosa Miguel, Cheng Jie-Fei
机构信息
Department of Chemistry, Tanabe Research Laboratories USA, Inc., 4540 Towne Centre Court, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5978-82. doi: 10.1016/j.bmcl.2007.07.071. Epub 2007 Aug 21.
Synthesis and structure-activity relationship of a series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitrile derivatives as EGFR inhibitors is described. Compounds 29 and 30 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the functional cellular assay. They are moderately selective against other types of tyrosine kinases.
描述了一系列作为表皮生长因子受体（EGFR）抑制剂的4-（2-芳基-环丙基氨基）-喹啉-3-腈衍生物的合成及其构效关系。化合物29和30在酶分析以及细胞功能分析中均显示出有效的体外抑制活性。它们对其他类型的酪氨酸激酶具有适度的选择性。
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