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
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| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2014-05 |
| 卷号 | 5期号:5页码:592-597 |
| 关键词 | Angiogenesis HUVEC inhibitor naphthamide VEGFR-2 |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/ml5000417 |
| 文献子类 | Article |
| 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关键词 | ENDOTHELIAL GROWTH-FACTOR ; RENAL-CELL CARCINOMA ; FACTOR RECEPTOR ; CANCER ; ANGIOGENESIS ; DISEASE |
| 资助项目 | National Natural Science Foundation of China[81273365] ; National Natural Science Foundation of China[81173080] ; Major Projects in National Science and Technology "Creation of Major New Drugs"[2012ZX09103101-024] ; Shanghai Science and Technology Commission[11431921100] ; Shanghai Science and Technology Commission[12DZ1930802] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000335879300029 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277095]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物化学研究室 |
| 通讯作者 | Xie, Hua |
| 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：上海药物研究所
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