• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

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.

DOI:10.1016/j.bmcl.2007.07.071
PMID:17827009
Abstract

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.

摘要

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。

相似文献

1
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.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
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5978-82. doi: 10.1016/j.bmcl.2007.07.071. Epub 2007 Aug 21.
2
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.6,7-二取代-4-(芳基氨基)喹啉-3-腈作为人表皮生长因子受体-2激酶活性的口服活性不可逆抑制剂的优化
J Med Chem. 2005 Feb 24;48(4):1107-31. doi: 10.1021/jm040159c.
3
4-Anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles as potent Src kinase inhibitors.4-苯胺基-7,8-二烷氧基苯并[g]喹啉-3-腈作为有效的Src激酶抑制剂。
J Med Chem. 2005 Sep 22;48(19):5909-20. doi: 10.1021/jm050512u.
4
Synthesis and antiproliferative activity of tyrphostins containing quinoline moieties.含喹啉部分的 tyrphostins 的合成及抗增殖活性
Anticancer Drug Des. 1996 Sep;11(6):463-83.
5
Design, synthesis, and biological evaluation of substituted 2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylamine related compounds as fructose-1,6-bisphosphatase inhibitors.作为果糖-1,6-二磷酸酶抑制剂的取代2,3-二氢-1H-环戊并[b]喹啉-9-基胺相关化合物的设计、合成及生物学评价
Bioorg Med Chem. 2006 Dec 1;14(23):7846-53. doi: 10.1016/j.bmc.2006.07.059.
6
Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.用喹啉-3-腈抑制Tpl2激酶和肿瘤坏死因子α生成以治疗类风湿性关节炎。
Bioorg Med Chem Lett. 2006 Dec 1;16(23):6067-72. doi: 10.1016/j.bmcl.2006.08.102. Epub 2006 Sep 14.
7
Binding modes of 6,7 di-substituted 4-anilinoquinoline-3-carbonitriles to EGFR.6,7-二取代-4-苯胺基喹啉-3-腈与表皮生长因子受体（EGFR）的结合模式
Bioorg Med Chem Lett. 2004 Jul 5;14(13):3397-400. doi: 10.1016/j.bmcl.2004.04.080.
8
Synthesis and antiproliferative activity of unsaturated quinoline derivatives.不饱和喹啉衍生物的合成及其抗增殖活性
Anticancer Drug Des. 2000 Jun;15(3):171-81.
9
Specificity of alpha-cyano-beta-hydroxy-beta-methyl-n-[4-(trifluoromethoxy)phe nyl]-propenamide as an inhibitor of the epidermal growth factor receptor tyrosine kinase.α-氰基-β-羟基-β-甲基-N-[4-(三氟甲氧基)苯基]-丙烯酰胺作为表皮生长因子受体酪氨酸激酶抑制剂的特异性
Clin Cancer Res. 1999 Dec;5(12):4264-72.
10
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).6,7-二取代-4-苯胺基喹啉-3-腈的合成及其构效关系。一种口服活性、不可逆的表皮生长因子受体（EGFR）和人表皮生长因子受体2（HER-2）酪氨酸激酶活性抑制剂的设计。
J Med Chem. 2003 Jan 2;46(1):49-63. doi: 10.1021/jm020241c.

引用本文的文献

1
Unravelling the target landscape of tranylcypromines for new drug discovery.解析反苯环丙胺的靶点格局以用于新药研发。
Acta Pharm Sin B. 2025 Jun;15(6):2985-3007. doi: 10.1016/j.apsb.2025.04.012. Epub 2025 Apr 14.
2
Chiral iron porphyrin (+)-D-(por)FeCl catalyzes highly enantioselective cyclopropanation of alkenes using generated diazoacetonitrile with up to 35 000 product turnover.手性铁卟啉（+）-D-（卟）FeCl使用生成的重氮乙腈催化烯烃的高度对映选择性环丙烷化反应，产物转化率高达35000。
Chem Sci. 2025 Apr 11;16(17):7191-7202. doi: 10.1039/d5sc00461f. eCollection 2025 Apr 30.
3
Design, Synthesis and Biological Evaluation of and -like Double Warhead Quinolinones Bearing Dihydroxy Naphthalene Moiety as Epidermal Growth Factor Receptor Inhibitors with Potential Apoptotic Antiproliferative Action.
含二羟基萘部分的和类似双弹头喹啉酮作为表皮生长因子受体抑制剂的设计、合成与生物评价，具有潜在的促凋亡抗增殖作用。
Molecules. 2022 Dec 10;27(24):8765. doi: 10.3390/molecules27248765.
4
Discovery of VEGFR2 inhibitors by integrating naïve Bayesian classification, molecular docking and drug screening approaches.通过整合朴素贝叶斯分类、分子对接和药物筛选方法发现血管内皮生长因子受体2（VEGFR2）抑制剂
RSC Adv. 2018 Jan 30;8(10):5286-5297. doi: 10.1039/c7ra12259d. eCollection 2018 Jan 29.
5
2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights.2-芳基喹啉类作为新型具有双重 EGFR/FAK 激酶抑制活性的抗癌剂：合成、生物评价和分子模拟见解。
J Enzyme Inhib Med Chem. 2022 Dec;37(1):349-372. doi: 10.1080/14756366.2021.2015344.
6
Discovery of 4-alkoxy-2-aryl-6,7-dimethoxyquinolines as a new class of topoisomerase I inhibitors endowed with potent in vitro anticancer activity.发现 4-烷氧基-2-芳基-6,7-二甲氧基喹啉类化合物作为一类新型拓扑异构酶 I 抑制剂，具有很强的体外抗癌活性。
Eur J Med Chem. 2021 Apr 5;215:113261. doi: 10.1016/j.ejmech.2021.113261. Epub 2021 Feb 9.
7
Quinoline-Based Molecules Targeting c-Met, EGF, and VEGF Receptors and the Proteins Involved in Related Carcinogenic Pathways.基于喹啉的分子靶向 c-Met、EGF 和 VEGF 受体以及相关致癌途径中的相关蛋白。
Molecules. 2020 Sep 18;25(18):4279. doi: 10.3390/molecules25184279.
8
Synthesis of some novel 2-(3-cyano -6-(thiophen- 2-yl)-4,4'- bipyridin-2- yloxy)acetohydrazide derivatives: assessment of their cytotoxic activity.一些新型2-(3-氰基-6-(噻吩-2-基)-4,4'-联吡啶-2-基氧基)乙酰肼衍生物的合成：其细胞毒性活性评估
BMC Chem. 2020 Jun 2;14(1):40. doi: 10.1186/s13065-020-00692-4. eCollection 2020 Dec.
9
Synthesis and X-ray study of dispiro 8-nitroquinolone analogues and their cytotoxic properties against human cervical cancer HeLa cells.双螺环8-硝基喹诺酮类似物的合成、X射线研究及其对人宫颈癌HeLa细胞的细胞毒性特性
Medchemcomm. 2019 Jan 22;10(3):439-449. doi: 10.1039/c8md00482j. eCollection 2019 Mar 1.
10
New arylated benzo[h]quinolines induce anti-cancer activity by oxidative stress-mediated DNA damage.新型芳基苯并[h]喹啉通过氧化应激介导的 DNA 损伤诱导抗癌活性。
Sci Rep. 2016 Dec 6;6:38128. doi: 10.1038/srep38128.