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Discovery of a new series of naphthamides as potent VEGFR-2 kinase inhibitors

ACS Medicinal Chemistry Letters, ISSN: 1948-5875, Vol: 5, Issue: 5, Page: 592-597
2014
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Article Description

Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer. In this study, we describe the design, synthesis, and biological evaluation of a new series of naphthamides as potent inhibitors of VEGFR-2. Among these compounds, 14c exhibited high VEGFR-2 inhibitory potency in both enzymatic and HUVEC cellular proliferation assays, with IC values of 1.5 and 0.9 nM, respectively. Kinase selectivity profiling revealed that 14c was a multitargeted inhibitor, and it also exhibited good potency against VEGFR-1, PDGFR-β, and RET. Furthermore, 14c effectively blocked tube formation of HUVEC at nanomolar level. Overall, 14c might be a promising candidate for the treatment of cancer. © 2014 American Chemical Society.

Bibliographic Details

Lv, Yongcong; Li, Mengyuan; Liu, Ting; Tong, Linjiang; Peng, Ting; Wei, Lixin; Ding, Jian; Xie, Hua; Duan, Wenhu

American Chemical Society (ACS)

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics; Chemistry

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