Journal
MOLECULES
Volume 22, Issue 10, Pages -Publisher
MDPI AG
DOI: 10.3390/molecules22101624
Keywords
EGFR; tyrosine kinase inhibitor; synthesis; 4-stilbenylamino-4(3H)-quinazoline; antitumor agents
Funding
- National Natural Science Foundation of China [21706209]
- Natural Science Foundation of Shaanxi Province [2017JQ2028]
- Key Industrial Research Project of Shaanxi Province [2017GY-126]
- Natural Science Foundation of Education Department of Shaanxi Province [15JK2148, 15JK2152]
- Special Natural Science Foundation of Science and Technology Bureau of Xi'an City [CXY1443WL21, 2016CXWL10]
- Xi'an Engineering Research Center of Environmental Detection and Food Safety [2016105GG/ZT05(4)]
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In an attempt to explore a new class of epidermal growth factor receptor (EGFR) inhibitors, novel 4-stilbenylamino quinazoline derivatives were synthesized through a Dimorth rearrangement reaction and characterized via IR, H-1-NMR, C-13-NMR, and HRMS. Methoxyl, methyl, halogen, and trifluoromethyl groups on stilbeneamino were detected. These synthesized compounds were evaluated for antitumor activity in vitro against eight human tumor cell lines with an MTS assay. Most synthesized compounds exhibited more potent activity (IC50 = similar to 2.0 mu M) than gefitinib (IC50 > 10.0 mu M) against the A431, A549, and BGC-823 cell lines. Docking methodology of compound 6c and 6i binding into the ATP site of EGFR was carried out. The results showed that fluorine and trifluoromethyl played an important role in efficient cell activity.
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