Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors

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	Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors
	Lv, Yongcong ; Li, Mengyuan ; Liu, Ting ; Tong, Linjiang ; Peng, Ting ; Wei, Lixin ; Ding, Jian ; Xie, Hua ; Duan, Wenhu
	2014-05-01
发表期刊	ACS MEDICINAL CHEMISTRY LETTERS ; Lv, YC; Li, MY; Liu, T; Tong, LJ; Peng, T; Wei, LX; Ding, J; Xie, H; Duan, WH.Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors,ACS MEDICINAL CHEMISTRY LETTERS,2014,5(5):592
摘要	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 IC50 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-beta, 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.; 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 IC50 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-beta, 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.
文献类型	期刊论文
条目标识符	http://210.75.249.4/handle/363003/32292
专题	中国科学院西北高原生物研究所
推荐引用方式 GB/T 7714	Lv, Yongcong,Li, Mengyuan,Liu, Ting,et al. Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors[J]. ACS MEDICINAL CHEMISTRY LETTERS, Lv, YC; Li, MY; Liu, T; Tong, LJ; Peng, T; Wei, LX; Ding, J; Xie, H; Duan, WH.Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors,ACS MEDICINAL CHEMISTRY LETTERS,2014,5(5):592,2014.
APA	Lv, Yongcong.,Li, Mengyuan.,Liu, Ting.,Tong, Linjiang.,Peng, Ting.,...&Duan, Wenhu.(2014).Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.ACS MEDICINAL CHEMISTRY LETTERS.
MLA	Lv, Yongcong,et al."Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors".ACS MEDICINAL CHEMISTRY LETTERS (2014).