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 ; Li, Meng-Yuan ; Tong, Lin-Jiang ; Wei, Li-Xin ; Ding, Jian ; Xie, Hua ; Duan, Wen-Hu
	2015-09-01
发表期刊	CHINESE CHEMICAL LETTERS
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.
文献类型	期刊论文
条目标识符	http://210.75.249.4/handle/363003/42777
专题	中国科学院西北高原生物研究所
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.
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.
MLA	Gao, Guo-Rui,et al."Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I)".CHINESE CHEMICAL LETTERS (2015).