New Journal of Chemistry p. 17203 - 17215 (2018)
Update date:2022-08-11
Topics:
OuYang, Yiqiang
Wang, Caolin
Zhao, Bingbing
Xiong, Hehua
Xiao, Zhen
Zhang, Bingliang
Zheng, Pengwu
Hu, Jiayi
Gao, Yanli
Zhang, Manli
Zhu, Wufu
Xu, Shan
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.
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