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Molecules 2018, 23(1), 24;

Design and Discovery of Quinazoline- and Thiourea-Containing Sorafenib Analogs as EGFR and VEGFR-2 Dual TK Inhibitors

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation ( Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 2 December 2017 / Revised: 19 December 2017 / Accepted: 21 December 2017 / Published: 23 December 2017
(This article belongs to the Section Medicinal Chemistry)
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Both EGFR and VEGFR-2 play a critical role in tumor growth, angiogenesis and metastasis, and targeting EGFR and VEGFR-2 simultaneously represents a promising approach to cancer treatment. In this work, a series of novel quinazoline- and thiourea-containing sorafenib analogs (10av) were designed and synthesized as EGFR and VEGFR-2 dual TK inhibitors. Their in vitro enzymatic inhibitory activities against EGFR and VEGFR-2, and antiproliferative activities against HCT-116, MCF-7 and B16 cell lines were evaluated and described. Most of the compounds showed potent activities against both cell lines and TK kinases. Compounds 10b and 10q which exhibited the most potent inhibitory activities against EGFR (IC50 = 0.02 µM and 0.01 µM, respectively), VEGFR-2 (IC50 = 0.05 µM and 0.08 µM, respectively), and good antiproliferative activities, also displayed competitive anti-tumor activities than sorafenib in vivo by B16 melanoma xenograft model test. View Full-Text
Keywords: quinazoline; thiourea; sorafenib; TK inhibitor; molecular docking quinazoline; thiourea; sorafenib; TK inhibitor; molecular docking

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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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Sun, S.; Zhang, J.; Wang, N.; Kong, X.; Fu, F.; Wang, H.; Yao, J. Design and Discovery of Quinazoline- and Thiourea-Containing Sorafenib Analogs as EGFR and VEGFR-2 Dual TK Inhibitors. Molecules 2018, 23, 24.

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