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Molecules 2017, 22(10), 1624;

Design, Synthesis, and Antitumor Activity of Novel Quinazoline Derivatives

School of Chemical Engineering, The Key Laboratory for Surface Engineering and Remanufacturing in Shaanxi Province, Xi’an University, Xi’an 710065, China
School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi’an 710062, China
College of Chemistry and Chemical Engineering, Taiyuan University of Technology, Taiyuan 030024, China
Author to whom correspondence should be addressed.
Received: 28 August 2017 / Revised: 16 September 2017 / Accepted: 26 September 2017 / Published: 28 September 2017
(This article belongs to the Section Bioorganic Chemistry)
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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, 1H-NMR, 13C-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 = ~2.0 μM) than gefitinib (IC50 > 10.0 μM) 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. View Full-Text
Keywords: EGFR; tyrosine kinase inhibitor; synthesis; 4-stilbenylamino-4(3H)-quinazoline; antitumor agents EGFR; tyrosine kinase inhibitor; synthesis; 4-stilbenylamino-4(3H)-quinazoline; antitumor agents

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Wang, L.; Li, P.; Li, B.; Wang, Y.; Li, J.; Song, L. Design, Synthesis, and Antitumor Activity of Novel Quinazoline Derivatives. Molecules 2017, 22, 1624.

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