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Molecules 2017, 22(10), 1624; doi:10.3390/molecules22101624

Design, Synthesis, and Antitumor Activity of Novel Quinazoline Derivatives

1
School of Chemical Engineering, The Key Laboratory for Surface Engineering and Remanufacturing in Shaanxi Province, Xi’an University, Xi’an 710065, China
2
School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi’an 710062, China
3
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)
View Full-Text   |   Download PDF [1230 KB, uploaded 28 September 2017]   |  

Abstract

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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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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