Novel tricyclic azepine derivatives: Biological evaluation of pyrimido(4,5-b)-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase.

Smith L 2nd; Wong WC; Kiselyov AS; Burdzovic Wizemann S; Mao Y; Xu Y; Duncton MA; Kim K; Piatnitski EL; Doody JF; Wang Y; Rosler RL; Milligan D; Columbus J; Balagtas C; Lee SP; Konovalov A; Hadari YR

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Novel tricyclic azepine derivatives: Biological evaluation of pyrimido(4,5-b)-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase.

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Novel tricyclic azepine derivatives: Biological evaluation of pyrimido(4,5-b)-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase.

机译：新型三环a庚因衍生物：作为表皮生长因子受体酪氨酸激酶抑制剂的嘧啶并（4,5-b）-1,4-苯并x庚因，硫氮平和二氮卓的生物学评估。

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Novel tricyclic derivatives containing an oxazepine, thiazepine, or diazepine ring were studied for their EGFR tyrosine kinase inhibitory activity. While the oxazepines were in general more potent than thiazepines, the diazepines displayed somewhat different structure-activity relationships. Moreover, the diazepines, in contrast to the oxazepines, showed appreciable inhibitory activity against the KDR tyrosine kinase. Furthermore, both oxazepines and diazepines demonstrated significant ability to inhibit autophosphorylation of EGFR in DiFi cells (generally, IC(50) values in the single-digit micromolar to submicromolar range).

机译：研究了含有氧杂氮平，硫氮平或二氮杂环的新型三环衍生物的EGFR酪氨酸激酶抑制活性。一般而言，奥氮平的功效比硫氮平强，但二氮卓的结构活性关系却有所不同。此外，与氧杂西平相反，二氮杂显示出对KDR酪氨酸激酶的明显抑制活性。此外，奥氮平和二氮卓均显示出显着的抑制DiFi细胞中EGFR自身磷酸化的能力（通常，IC（50）值在单位个微摩尔至亚微摩尔范围内）。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2006年第19期|共5页
作者
Smith L 2nd; Wong WC; Kiselyov AS; Burdzovic Wizemann S; Mao Y; Xu Y; Duncton MA; Kim K; Piatnitski EL; Doody JF; Wang Y; Rosler RL; Milligan D; Columbus J; Balagtas C; Lee SP; Konovalov A; Hadari YR;
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正文语种 eng
中图分类基础医学;
关键词
diazepine; derivatives; Protein-Tyrosine Kinase; 蛋白质酪氨酸激酶;

机译：diazepine;derivatives;Protein-Tyrosine Kinase;蛋白质酪氨酸激酶;

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1. Novel tricyclic azepine derivatives: Biological evaluation of pyrimido(4,5-b)-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase. [J] . Smith L 2nd, Wong WC, Kiselyov AS, Bioorganic and Medicinal Chemistry Letters . 2006,第19期

机译：新型三环a庚因衍生物：作为表皮生长因子受体酪氨酸激酶抑制剂的嘧啶并（4,5-b）-1,4-苯并x庚因，硫氮平和二氮卓的生物学评估。
2. Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno3, 2-dpyrimidines and pyrimido5,4-b- and -4,5-bindoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase. [J] . Showalter HD, Bridges AJ, Zhou H, Journal of Medicinal Chemistry . 1999,第26期

机译：酪氨酸激酶抑制剂。 16.作为表皮生长因子受体酪氨酸激酶的有效抑制剂的6,5,6-三环苯并硫杂3，2-嘧啶和嘧啶5,4-b-和-4,5-联苯二酚。
3. Design, Synthesis and Biological Evaluation of the Quinazoline Derivatives as L858R/T790M/C797S Triple Mutant Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors [J] . Mingguang Zhang, Yunyun Wang, Jia Wang, Chemical and Pharmaceutical Bulletin . 2020,第10期

机译：喹唑啉衍生物的设计，合成和生物学评价为L858R / T790M / C797S三重突变表皮生长因子受体酪氨酸激酶抑制剂
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. >Association Of Initial Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors Treatment And EGFR Exon 19 Deletion With Frequency Of The T790M Mutation In Non-Small Cell Lung Cancer Patients After Resistance To First-Line Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors [O] . Wen Gao, Jing He, Shi-Dai Jin, 2019

机译：>初始表皮生长因子受体酪氨酸激酶抑制剂治疗和EGFR外显子抑制剂的抗血液抗性抗血液肺癌患者T790M突变抗性抗性后，抗抗血疱剂患者的抗性，抗抗血管生长因子受体酪氨酸激酶抑制剂

Novel tricyclic azepine derivatives: Biological evaluation of pyrimido(4,5-b)-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase.

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