Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I) | |
Gao, Guo-Rui1; Li, Meng-Yuan2,3; Tong, Lin-Jiang2; Wei, Li-Xin3; Ding, Jian2; Xie, Hua2; Duan, Wen-Hu1,4 | |
刊名 | chinese chemical letters
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2015-09-01 | |
卷号 | 26期号:9页码:1165-1168 |
关键词 | VEGFR-2 Inhibitor Indole |
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 series of o-linked indoles as potent inhibitors of vegfr-2. among these compounds, 18 showed significant anti-angiogenesis activities via vegfr-2 in enzymatic proliferation assays, with ic50 value of 3.8 nmol/l. kinase selectivity profiling revealed that 18 was a multitargeted inhibitor, and it also exhibited good potency against vegfr-1, pdgfr-alpha and beta. (c) 2015 chinese chemical society and institute of materia medica, chinese academy of medical sciences. published by elsevier b.v. all rights reserved. |
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 series of o-linked indoles as potent inhibitors of vegfr-2. among these compounds, 18 showed significant anti-angiogenesis activities via vegfr-2 in enzymatic proliferation assays, with ic50 value of 3.8 nmol/l. kinase selectivity profiling revealed that 18 was a multitargeted inhibitor, and it also exhibited good potency against vegfr-1, pdgfr-alpha and beta. (c) 2015 chinese chemical society and institute of materia medica, chinese academy of medical sciences. published by elsevier b.v. all rights reserved. |
WOS标题词 | science & technology ; physical sciences |
类目[WOS] | chemistry, multidisciplinary |
研究领域[WOS] | chemistry |
关键词[WOS] | endothelial growth-factor ; hepatocellular-carcinoma ; factor receptor ; cancer ; potent |
收录类别 | SCI |
语种 | 英语 |
WOS记录号 | WOS:000361407700025 |
内容类型 | 期刊论文 |
源URL | [http://ir.nwipb.ac.cn/handle/363003/5515] ![]() |
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.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Northwest Inst Plateau Biol, Pharmacol & Safety Evaluat Key Lab Tibetan Med Qi, Xining 810008, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China |
推荐引用方式 GB/T 7714 | Gao, Guo-Rui,Li, Meng-Yuan,Tong, Lin-Jiang,et al. Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I)[J]. chinese chemical letters,2015,26(9):1165-1168. |
APA | Gao, Guo-Rui.,Li, Meng-Yuan.,Tong, Lin-Jiang.,Wei, Li-Xin.,Ding, Jian.,...&Duan, Wen-Hu.(2015).Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I).chinese chemical letters,26(9),1165-1168. |
MLA | Gao, Guo-Rui,et al."Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I)".chinese chemical letters 26.9(2015):1165-1168. |
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