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Molecules 2016, 21(11), 1572; doi:10.3390/molecules21111572

Design, Synthesis and Structure-Activity Relationships of Novel Diaryl Urea Derivatives as Potential EGFR Inhibitors

Key Lab. of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, China
Department of Chemsitry, Shenyang Medical College, 146 Huanghe North Street, Huanggu District, Shenyang 110034, China
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 19 October 2016 / Revised: 11 November 2016 / Accepted: 15 November 2016 / Published: 18 November 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1756 KB, uploaded 18 November 2016]   |  


Two novel series of diaryl urea derivatives 5ai and 13al were synthesized and evaluated for their cytotoxicity against H-460, HT-29, A549, and MDA-MB-231 cancer cell lines in vitro. Therein, 4-aminoquinazolinyl-diaryl urea derivatives 5ai demonstrated significant activity, and seven of them are more active than sorafenib, with IC50 values ranging from 0.089 to 5.46 μM. Especially, compound 5a exhibited the most active potency both in cellular (IC50 = 0.15, 0.089, 0.36, and 0.75 μM, respectively) and enzymatic assay (IC50 = 56 nM against EGFR), representing a promising lead for further optimization. View Full-Text
Keywords: diaryl urea; 4-aminoquinazolinyl; synthesis; cytotoxicity; EGFR inhibitors diaryl urea; 4-aminoquinazolinyl; synthesis; cytotoxicity; EGFR inhibitors

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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Jiang, N.; Bu, Y.; Wang, Y.; Nie, M.; Zhang, D.; Zhai, X. Design, Synthesis and Structure-Activity Relationships of Novel Diaryl Urea Derivatives as Potential EGFR Inhibitors. Molecules 2016, 21, 1572.

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