Bioorganic and Medicinal Chemistry p. 6084 - 6091 (2013)
Update date:2022-08-05
Topics:
Xu, Yun-Yun
Li, Si-Ning
Yu, Gao-Jian
Hu, Qing-Hua
Li, Huan-Qiu
Two new series of new compounds containing a 6-amino-substituted group or 6-acrylamide-substituted group linked to a 4-anilinoquinazoline nucleus have been discovered as potential EGFR inhibitors. These compounds proved efficient effects on antiproliferative activity and EGFR-TK inhibitory activity. Especially, N6-((5-bromothiophen-2-yl)methyl)-N4-(3- chlorophenyl)quinazoline-4,6-diamine (5e), showed the most potent inhibitory activity (IC50 = 3.11 μM for Hep G2, IC50 = 0.82 μM for A549). The EGFR molecular docking model suggested that the new compound is nicely bound to the region of EGFR, and cell morphology by Hoechst stain experiment suggested that these compounds efficiently induced apoptosis of A549 cells.
View MoreWeifang Jahwa Chemical Co.,Ltd
Contact:0086-536-8897731,8897730
Address:No.5166 East Dongfeng Street,Weifang,Shandong,China
SHOUGUANG BOYU CHEMICAL CO.,LTD
Contact:+86-536-8256719
Address:ROOM 1101&1103,BUILDING D,ZHONGTU MANSION,NO.6565 EAST FUSHOU STREET,WEIFANG CITY,SHANDONG,CHINA.
Contact:+86-21-6856-1349 523-87676172
Address:No16 . BinJiang Road . Taixing Economy Developing Area .JiangSu Province . China
Hefei EnliPharma Tecnology Co.,Ltd
Contact:0086-551-66399836
Address:Qing Cheng ShuiXiang Building 805, Mengcheng North Road , ShuangFeng Economic Development Zone Anhui HeFei
Tianjin Bright Future Technology Co., Ltd
Contact:0086-22-58016666
Address:NO.136 DongTeng Lake Street Tianjin Economic and Technology Development Area,Tainjin,China
Doi:10.1016/S0022-328X(00)81948-8
(1982)Doi:10.1021/jo50017a014
(1953)Doi:10.1007/BF01150910
(1992)Doi:10.1007/s11172-013-0065-6
()Doi:10.1016/j.tet.2006.07.051
(2006)Doi:10.1002/jhet.5570200113
(1983)