Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors
文献类型：期刊论文
| 作者 | Lv, Yongcong1; Li, Mengyuan2,3; Liu, Ting1,4; Tong, Linjiang2; Peng, Ting2; Wei, Lixin3; Ding, Jian2; Xie, Hua2; Duan, Wenhu1 |
| 刊名 | acs medicinal chemistry letters
 |
| 出版日期 | 2014-05-01 |
| 卷号 | 5期号:5页码:592-597 |
| 关键词 | Angiogenesis HUVEC inhibitor naphthamide VEGFR-2 |
| ISSN号 | 1948-5875 |
| 中文摘要 | 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. |
| 英文摘要 | 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. |
| WOS标题词 | science & technology ; life sciences & biomedicine |
| 类目[WOS] | chemistry, medicinal |
| 研究领域[WOS] | pharmacology & pharmacy |
| 关键词[WOS] | endothelial growth-factor ; renal-cell carcinoma ; factor receptor ; cancer ; angiogenesis ; disease |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS记录号 | WOS:000335879300029 |
| 公开日期 | 2014-12-19 |
| 源URL | [http://ir.nwipb.ac.cn/handle/363003/4236]  |
| 专题 | 西北高原生物研究所_中国科学院西北高原生物研究所 |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Northwest Inst Plateau Biol, Qinghai 81008, Peoples R China 4.Nanchang Univ, Coll Med, Nanchang 330066, Jiangxi, Peoples R China |
| 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,2014,5(5):592-597. |
| 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,5(5),592-597. |
| MLA | Lv, Yongcong,et al."Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors".acs medicinal chemistry letters 5.5(2014):592-597. |
入库方式： OAI收割
来源：西北高原生物研究所
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