期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 19, 页码 6084-6091出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.06.070
关键词
EGFR-TK inhibitors; 4-Anilinoquinazoline; Antitumor; Molecular docking
资金
- National Natural Science Foundation of China [81102316]
- Natural Science Foundation of the Jiangsu Higher Education Institutions of China [11KJD350002]
- PAPD
- Priority Academic Program Development of Jiangsu Higher Education Institutions
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, N-6-((5-bromothiophen-2-yl) methyl)-N-4-(3-chlorophenyl) quinazoline-4,6-diamine (5e), showed the most potent inhibitory activity (IC50 = 3.11 mu M for Hep G2, IC50 = 0.82 mu M 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. (c) 2013 Elsevier Ltd. All rights reserved.
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