Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.

Luth A; Lowe W

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Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.

机译：4-（吲哚-3-基）喹唑啉的合成：一类新的表皮生长因子受体酪氨酸激酶抑制剂。

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The epidermal growth factor (EGF) family of membrane receptors has been identified as a key element in the complex signaling network that is utilized by various classes of cell-surface receptors. The synthesis and pharmacological results of 4-(indole-3-yl)quinazolines are described. The synthesized compounds are new high potent EGFR-tyrosine kinase inhibitors with excellent cytotoxic properties at different cell lines. Furthermore the 4-(indole-3-yl)quinazolines show some tendencies to inhibit the HER-2 TK, too. Moreover this substance class has remarkable strong fluorescence properties.

机译：膜受体的表皮生长因子（EGF）家族已被确定为复杂信号网络中的关键元素，该信号网络被各种类型的细胞表面受体所利用。描述了4-（吲哚-3-基）喹唑啉的合成和药理结果。合成的化合物是新型高效的EGFR-酪氨酸激酶抑制剂，在不同细胞系中均具有优异的细胞毒性。此外，4-（吲哚-3-基）喹唑啉也显示出一些抑制HER-2 TK的趋势。此外，该物质类别具有显着的强荧光特性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2008年第7期|共11页
作者
Luth A; Lowe W;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词
Quinazolines; indole; inhibitors; Protein-Tyrosine Kinase; Epidermal Growth Factor; 喹唑啉类; 蛋白质酪氨酸激酶;

机译：Quinazolines;indole;inhibitors;Protein-Tyrosine Kinase;Epidermal Growth Factor;喹唑啉类;蛋白质酪氨酸激酶;

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1. Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors. [J] . Luth A, Lowe W European Journal of Medicinal Chemistry: Chimie Therapeutique . 2008,第7期

机译：4-（吲哚-3-基）喹唑啉的合成：一类新的表皮生长因子受体酪氨酸激酶抑制剂。
2. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions [J] . Smaill JB., Loo JA., Greis KD., Journal of Medicinal Chemistry . 2000,第7期

机译：酪氨酸激酶抑制剂。 17.表皮生长因子受体的不可逆抑制剂：4-（苯基氨基）喹唑啉-和4-（苯基氨基）吡啶并[3,2-d]嘧啶-6-丙烯酰胺，具有额外的增溶功能
3. Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido(d)pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. [J] . Smaill JB, Palmer BD, Rewcastle GW, Journal of Medicinal Chemistry . 1999,第10期

机译：酪氨酸激酶抑制剂。 15.作为表皮生长因子受体的ATP结合位点的不可逆抑制剂的4-（苯基氨基）喹唑啉和4-（苯基氨基）吡啶基（d）嘧啶丙烯酰胺。
4. QSAR Study of Quinazoline Derivatives as Inhibitor of Epidermal Growth Factor Receptor-Tyrosine Kinase (EGFR-TK) [C] . La Ode Aman, Widisusanti Abdulkadir, Julitha Geybie Rembet, International Conference on Computation for Science and Technology . 2015

机译：喹唑啉衍生物作为表皮生长因子受体 - 酪氨酸激酶（EGFR-TK）抑制剂的QSAR研究
5. Unanticipated Effects of Tyrosine Kinase Inhibitors on Vitamin D Receptor Expression and Gene Regulation In Epidermal Growth Factor Receptor-Mutated Non-Small Cell Lung Cancer. [D] . Timberlake, Alexandra F. 2017

机译：酪氨酸激酶抑制剂对表皮生长因子受体突变的非小细胞肺癌中维生素D受体表达和基因调控的意外影响。
6. Sensitivities to various epidermal growth factor receptor‐tyrosine kinase inhibitors of uncommon epidermal growth factor receptor mutations L861Q and S768I: What is the optimal epidermal growth factor receptor‐tyrosine kinase inhibitor? [O] . Eri Banno, Yosuke Togashi, Yu Nakamura, 2016

机译：对各种表皮生长因子受体酪氨酸激酶抑制剂的罕见表皮生长因子受体突变L861Q和S768I的敏感性：最佳的表皮生长因子受体酪氨酸激酶抑制剂是什么？
7. Baseline and Trend of Lymphocyte-to-Monocyte Ratio as Prognostic Factors in Epidermal Growth Factor Receptor Mutant Non-Small Cell Lung Cancer Patients Treated with First-Line Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors. [O] . Yu-Mu Chen, Chien-Hao Lai, Huang-Chih Chang, 2015

机译：淋巴细胞与单核细胞比率的基线和趋势作为表皮生长因子受体突变非小细胞肺癌患者用一线表皮生长因子受体酪氨酸激酶抑制剂治疗的预后因素。

Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.

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