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Molecules 2015, 20(10), 19361-19371;

Design, Synthesis, Activity and Docking Study of Sorafenib Analogs Bearing Sulfonylurea Unit

School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, China
Jiangxi Province Institute of Materia Medica, Nanchang 330000, China
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 10 August 2015 / Revised: 21 September 2015 / Accepted: 21 September 2015 / Published: 23 October 2015
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Two series of novel sorafenib analogs containing a sulfonylurea unit were synthesized and their chemical structures were confirmed by 1H-NMR, 13C-NMR, MS spectrum and elemental analysis. The synthesized compounds were evaluated for the cytotoxicity against A549, Hela, MCF-7, and PC-3 cancer cell lines. Some of the compounds showed moderate cytotoxic activity, especially compounds 1-(2,4-difluorophenylsulfonyl)-3-(4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea (6c) and 1-(4-bromophenylsulfonyl)-3-(4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea (6f) with the IC50 values against four cancer cell lines ranging from 16.54 ± 1.22 to 63.92 ± 1.81 μM, respectively. Inhibitory rates against vascular endothelial growth factor receptor-2 (VEGFR2/KDR) kinase at 10 μM of target compounds were further carried out in this paper in order to investigate the target of these compounds. Structure-activity relationships (SARs) and docking studies indicated that the sulfonylurea unit was important to these kinds of compounds. None of the substitutions in the phenoxy group and small halogen atoms such as 2,4-difluoro substitution of the aryl group contributed to the activity. The results suggested that sulfonylurea sorafenib analogs are worthy of further study. View Full-Text
Keywords: sorafenib; sulfonylurea; VEGFR2/KDR kinase inhibitors; anticancer activity sorafenib; sulfonylurea; VEGFR2/KDR kinase inhibitors; anticancer activity

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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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Wu, C.; Wang, M.; Tang, Q.; Luo, R.; Chen, L.; Zheng, P.; Zhu, W. Design, Synthesis, Activity and Docking Study of Sorafenib Analogs Bearing Sulfonylurea Unit. Molecules 2015, 20, 19361-19371.

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