Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing oxazole or imidazole as potential EGFR inhibitors
| Autor: | Manli Zhang, Bingliang Zhang, Hehua Xiong, Zhen Xiao, Jiayi Hu, Bingbing Zhao, Caolin Wang, Ouyang Yiqiang, Pengwu Zheng, Wufu Zhu, Yanli Gao, Shan Xu |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
A549 cell Stereochemistry Kinase Acridine orange General Chemistry Catalysis 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology 0302 clinical medicine chemistry Apoptosis Docking (molecular) 030220 oncology & carcinogenesis Materials Chemistry Imidazole Propidium iodide Oxazole |
| Zdroj: | New Journal of Chemistry. 42:17203-17215 |
| ISSN: | 1369-9261 1144-0546 |
| DOI: | 10.1039/c8nj03594f |
| Popis: | Six series of quinazoline derivatives bearing oxazole or imidazole (8a–f, 9a–f, 10a–d, 11a–f, 12a–d and 13a–i) were designed, synthesized and their IC50 values evaluated against three cancer cell lines (A549, MCF-7 and PC-3). Most of the thirty-five target compounds showed excellent antiproliferative activity against one or several cancer cell lines. Compound 12a showed the best activity against A549, MCF-7 and PC-3 cancer cell lines, with IC50 values of 1.90 ± 0.13 μM, 2.23 ± 0.28 μM and 2.03 ± 0.14 μM, respectively. Four selected compounds (8a, 9d, 10a and 12a) were further evaluated for the inhibitory activity against EGFR kinase. AnnexinV-FITC, propidium iodide (PI) double staining and acridine orange single staining results indicated that compound 12a could induce apoptosis of human lung cancer A549 cells. |
| Databáze: | OpenAIRE |
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