Design, Synthesis, and Biological Evaluation of Sorafenib Analogs Bearing a Sulfonylurea Unit as Novel VEGFR2 Kinase Inhibitors

Wu Fu Zhu; Chun Jiang Wu; Shan Xu; Wei Li; Hai Hong Fang; Zhi Chao Chen; Xu Huang Tu; Peng Wu Zheng

doi:10.4028/www.scientific.net/AMR.989-994.1048

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HomeAdvanced Materials ResearchAdvanced Materials Research Vols. 989-994Design, Synthesis, and Biological Evaluation of...

Design, Synthesis, and Biological Evaluation of Sorafenib Analogs Bearing a Sulfonylurea Unit as Novel VEGFR2 Kinase Inhibitors

Abstract:

Two sorafenib analogs (9a,9b) containing sulfonylurea unit were synthesized and their chemical structures were confirmed by 1H NMR and MS spectrum. The synthesized compounds were evaluated for the inhibition rate against VEGFR2 kinase at 10μM level. The inhibition rates of compound 9a and 9b against VEGFR2 kinase were 61.0±11.1% and 22.6±2.6%, respectively. The results showed that the introduction of sulfonylurea unit is favorable for the activity, and further study is being carried out.

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Periodical:

Advanced Materials Research (Volumes 989-994)

Pages:

1048-1051

DOI:

https://doi.org/10.4028/www.scientific.net/AMR.989-994.1048

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Online since:

July 2014

Authors:

Wu Fu Zhu*, Chun Jiang Wu, Shan Xu, Wei Li, Hai Hong Fang, Zhi Chao Chen, Xu Huang Tu, Peng Wu Zheng

Keywords:

Anticancer Activity, Sorafenib, Sulfonylurea, VEGFR2 Kinase Inhibitors

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References

[1] Zhu W, Liu Y, Zhai X, et al. Design, synthesis and 3D-QSAR analysis of novel 2-hydrazinyl-4-morpholinothieno [3, 2-d] pyrimidine derivatives as potential antitumor agents, Euro. J. Med. Chem. 57(2012) 162-175.

DOI: 10.1016/j.ejmech.2012.09.002

Google Scholar

[2] Guida T, Anaganti S, Provitera L, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor β gatekeeper mutants. Clin. Cancer Res. 13(2007) 3363-3369.

DOI: 10.1158/1078-0432.ccr-06-2667

Google Scholar

[3] Barbosa M L C, Lima L M, Tesch R, et al. Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors[J]. Euro. J. Med. Chem. 71(2014) 1-14.

DOI: 10.1016/j.ejmech.2013.10.058

Google Scholar

[4] Yao J, He Z, Chen J, et al. Design, synthesis and biological activities of sorafenib derivatives as antitumor agents[J]. Bioorg. Med. Chem. Lett. 22(2012) 6549-6553.

DOI: 10.1016/j.bmcl.2012.09.031

Google Scholar

[5] M Logers, R Gehring, O Kuhn and M Matthaus, WO. Patent 2006034796. (2006).

Google Scholar

[6] Scarborough, M Robert. WO. Patent 2007056219A1. (2007).

Google Scholar

[7] Tsai, Henry J. D-420720, a novel orally active sulfonamide compound dipeptidylpeptidase inhibitor: structure and activity relationship of arylsulfonamide to dipeptidylpeptidase inhibitor[J]. Drug Develop. Res. 69(2008) 514-519.

DOI: 10.1002/ddr.20278

Google Scholar