European Journal of Medicinal Chemistry p. 29 - 43 (2018)
Update date:2022-08-02
Topics:
OuYang, Yiqiang
Zou, Wensheng
Peng, Liang
Yang, Zunhua
Tang, Qidong
Chen, Mengzi
Jia, Shuang
Zhang, Hong
Lan, Zhou
Zheng, Pengwu
Zhu, Wufu
Eight series of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline were designed, synthesized and evaluated for the IC50 values against three cancer cell lines (A549, MCF-7 and PC-3). Most of the forty nine target compounds showed excellent antiproliferative activity against one or several cancer cell lines. The compound 13a showed the best activity against A549, MCF-7 and PC-3 cancer cell lines, with the IC50 values of 1.09 ± 0.04 μM, 1.34 ± 0.13 μM and 1.23 ± 0.09 μM, respectively. Eight selected compounds were further selected to evaluated for the inhibitory activity against EGFR kinase. Three of them showed equal activity against EGFR kinase to positive control afatinib. AnnexinV-FITC, propidium iodide (PI) double staining and acridine orange single staining results indicated that the compound 13a could induce apoptosis of human lung cancer A549 cells.
View MoreContact:
Address:ROOM 1715, No#345 Jin Xiang Road, Pudong District
Nantong LiKai Chemical Co.,Ltd
Contact:+86-513-89068669
Address:Jincheng Science Park
Ji'an Kexin Trade Co., Ltd.(expird)
Contact:86-0796-8187704 18507063190
Address:ji'an jiangxi
Contact:+86-134-5286-9121
Address:Add: Wing Tuck Commercial Centre, 177-183 Wing Lok Street, Hong Kong,
HANGZHOU FOREWIN PHARMA CO., LTD
Contact:+86-571-89053961
Address:hangzhou
Doi:10.1246/bcsj.49.730
(1976)Doi:10.1021/acs.orglett.0c02465
(2020)Doi:10.1016/j.chemphyslip.2005.07.007
(2005)Doi:10.1016/S0040-4039(00)86229-2
(1983)Doi:10.1016/j.saa.2007.10.006
(2008)Doi:10.1007/s00044-005-0125-z
(2005)