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.
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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)