Design, synthesis, biological evaluation and docking study of novel quinazoline derivatives as EGFR-TK inhibitors
| Autor: | Rao Guowu, Zheng Quan, Jin Hao, Xiang-Zheng Tang, Wen Zhang, Hu Chenghai, Bai-Xu Wu |
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| Rok vydání: | 2021 |
| Předmět: |
Models
Molecular Cell Survival Antineoplastic Agents Apoptosis Benzazepine 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Docking (dog) Cell Line Tumor Drug Discovery Quinazoline Humans Protein Kinase Inhibitors Cell Proliferation 030304 developmental biology Biological evaluation EGFR inhibitors Pharmacology 0303 health sciences Quinazoline derivatives Molecular Structure Chemistry Combinatorial chemistry ErbB Receptors Design synthesis 030220 oncology & carcinogenesis Quinazolines Molecular Medicine Drug Screening Assays Antitumor |
| Zdroj: | Future Medicinal Chemistry. 13:601-612 |
| ISSN: | 1756-8927 1756-8919 |
| Popis: | Background: Quinazoline-based compounds have been proved effective in the treatment of cancers for years. Materials & methods: The structural features of several inhibitors of EGFR were integrated and quinazolines with a benzazepine moiety at the 4-position were constructed. Results: Most of the compounds exhibited excellent antitumor activities. Compound 33e showed excellent antitumor activities against the four tested cell lines (IC50: 1.06–3.55 μM). The enzymatic, signaling pathways and apoptosis assay of 33e were subsequently carried out to study the action of the mechanism. Conclusion: Compound 33e with a benzazepine moiety at the 4-position can be screened in this study and provides useful information for the design of EGFR-T790M inhibitors, which deserve additional research. |
| Databáze: | OpenAIRE |
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