Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I)

	Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I)
	Gao, Guo-Rui 1; Li, Meng-Yuan 2,3; Tong, Lin-Jiang 2; Wei, Li-Xin 3; Ding, Jian 2; Xie, Hua 2; Duan, Wen-Hu 1,4
刊名	chinese chemical letters
	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.