New substituted 4-arylaminoquinazolines as potent inhibitors of breast tumor cell lines: in vitro and docking experiments.

de Oliveira AN; Bocca CC; Carvalho JE; Ruiz AL; Silva TP; Rittner R; Hoehr NF

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New substituted 4-arylaminoquinazolines as potent inhibitors of breast tumor cell lines: in vitro and docking experiments.

机译：新的取代的4-芳基氨基喹唑啉类化合物作为乳腺肿瘤细胞系的有效抑制剂：体外和对接实验。

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The arylquinazolines represent significant advances in the clinical management of breast cancer. Nevertheless some confirmatory studies must be considered to foster the use of anti-EGFR therapies including safety and clinical use. Two 4-arylaminoquinazoline derivatives, recently synthesized, were tested as kinase inhibitors and their citotoxicities showed potent growth inhibitory activity in breast tumor cell lines (MCF-7). The predicted complex structure of quinazoline inhibitors with EGFR protein from molecular docking provided a stereoview of the binding site correlated with structure activity, affording important information about structure-based drug design.

机译：芳基喹唑啉代表了乳腺癌临床管理的重大进展。然而，必须考虑一些验证性研究以促进抗EGFR疗法的使用，包括安全性和临床使用。测试了最近合成的两种4-芳基氨基喹唑啉衍生物作为激酶抑制剂，它们的胞毒性显示了在乳腺癌细胞系（MCF-7）中的有效生长抑制活性。通过分子对接，预测的喹唑啉抑制剂与EGFR蛋白的复杂结构提供了与结构活性相关的结合位点的立体图，提供了有关基于结构的药物设计的重要信息。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第9期|共4页
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de Oliveira AN; Bocca CC; Carvalho JE; Ruiz AL; Silva TP; Rittner R; Hoehr NF;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. New substituted 4-arylaminoquinazolines as potent inhibitors of breast tumor cell lines: in vitro and docking experiments. [J] . de Oliveira AN, Bocca CC, Carvalho JE, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第9期

机译：新的取代的4-芳基氨基喹唑啉类化合物作为乳腺肿瘤细胞系的有效抑制剂：体外和对接实验。
2. Design,Syntheses,Biological Evaluation,and Docking Studies of 2-Substituted 5-Methylsulfonyl-1-Phenyl-1H-lndoles: Potent and Selective in vitro Cyclooxygenase-2 Inhibitors [J] . Olga Cruz-Lopez, Juan Jose Diaz-Mochon, Joaquin M.Campos ChemMedChem . 2007,第1期

机译：2-取代的5-甲基磺酰基-1-苯基-1H-吲哚类化合物的设计，合成，生物学评估和对接研究：有效且选择性的体外环氧合酶-2抑制剂
3. Antitumor activity of enzastaurin (LY317615.HCl) against human cancer cell lines and freshly explanted tumors investigated in in-vitro (corrected) soft-agar cloning experiments. [J] . Hanauske AR, Oberschmidt O, Hanauske-Abel H, Investigational new drugs. . 2007,第3期

机译：enzastaurin（LY317615.HCl）对人癌细胞系和新鲜移植的肿瘤的抗肿瘤活性在体外（校正的）软琼脂克隆实验中进行了研究。
4. IR spectroscopy and IR microscopy of human breast tumors xenografted breast tumors and breast tumor cell lines [C] . Heinz Fabian, Max-Delbrueck-Ctr. for Molecular Medicine, Berlin, Infrared Spectroscopy: New Tool in Medicine . 1998

机译：人乳腺肿瘤异种移植乳腺肿瘤和乳腺肿瘤细胞系的红外光谱和红外显微镜
5. Characterization of Mechanism(s) of Anti-Tumor Growth Exerted by Eosinophilic Cell Lines on Breast Tumor Cell Lines [D] . Laniyan, Ibrahim 2010

机译：嗜酸性细胞系对乳腺癌细胞系的抗肿瘤生长机制的表征
6. Trichlorobenzene-substituted azaaryl compounds as novel FGFR inhibitors exhibiting potent antitumor activity in bladder cancer cells in vitro and in vivo [O] . Chun-Han Chen, Yi-Min Liu, Shiow-Lin Pan, 2016

机译：作为新型FGFR抑制剂的三氯苯取代的氮杂芳基化合物在膀胱癌细胞中具有体内和体外有效的抗肿瘤活性
7. Green Tea Catechins Induce Inhibition of PTP1B Phosphatase in Breast Cancer Cells with Potent Anti-Cancer Properties: In Vitro Assay, Molecular Docking, and Dynamics Studies [O] . Alicja Kuban-Jankowska, Tomasz Kostrzewa, Claudia Musial, 2020

机译：绿茶儿茶素在乳腺癌细胞中诱导PTP1B磷酸酶，有效的抗癌性能：体外测定，分子对接和动力学研究

New substituted 4-arylaminoquinazolines as potent inhibitors of breast tumor cell lines: in vitro and docking experiments.

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