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

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	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
	2015-09-01
发表期刊	CHINESE CHEMICAL LETTERS
卷号	26 期号:9 页码:1165-1168
文章类型	Article
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.; 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.
关键词	Vegfr-2 Inhibitor Indole
WOS标题词	Science & Technology ; Physical Sciences
关键词[WOS]	ENDOTHELIAL GROWTH-FACTOR ; HEPATOCELLULAR-CARCINOMA ; FACTOR RECEPTOR ; CANCER ; POTENT
收录类别	SCI
语种	英语
WOS研究方向	Chemistry
WOS类目	Chemistry, Multidisciplinary
WOS记录号	WOS:000361407700025
引用统计	被引频次：9[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://210.75.249.4/handle/363003/5515
专题	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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