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Issue 7, 2015
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Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors

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Abstract

Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive strategy for the treatment of cancer. Herein, we describe the design, synthesis, and biological evaluation of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors. Among the new derivatives, compound 3k exhibited high VEGFR-2 inhibitory potency in both enzymatic and VEGF-induced HUVEC cellular proliferation assays (IC50 = 0.5 and 9.8 nM, respectively). Kinase selectivity profiling revealed that 3k was a highly selective VEGFR-2 inhibitor. Moreover, 3k effectively inhibited angiogenesis in HUVEC tube formationassay.

Graphical abstract: Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors

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Publication details

The article was received on 01 May 2015, accepted on 08 Jun 2015 and first published on 08 Jun 2015


Article type: Concise Article
DOI: 10.1039/C5MD00191A
Citation: Med. Chem. Commun., 2015,6, 1375-1380
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    Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors

    Y. Lv, M. Li, S. Cao, L. Tong, T. Peng, L. Wei, H. Xie, J. Ding and W. Duan, Med. Chem. Commun., 2015, 6, 1375
    DOI: 10.1039/C5MD00191A

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