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Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing oxazole or imidazole as potential EGFR inhibitors

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Abstract

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.

Graphical abstract: Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing oxazole or imidazole as potential EGFR inhibitors

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Publication details

The article was received on 19 Jul 2018, accepted on 04 Sep 2018 and first published on 05 Sep 2018


Article type: Paper
DOI: 10.1039/C8NJ03594F
Citation: New J. Chem., 2018, Advance Article
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    Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing oxazole or imidazole as potential EGFR inhibitors

    Y. OuYang, C. Wang, B. Zhao, H. Xiong, Z. Xiao, B. Zhang, P. Zheng, J. Hu, Y. Gao, M. Zhang, W. Zhu and S. Xu, New J. Chem., 2018, Advance Article , DOI: 10.1039/C8NJ03594F

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