Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors

	Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors
	Lv, Yongcong ; Li, Mengyuan ; Cao, Sufen ; Tong, Linjiang ; Peng, Ting ; Wei, Lixin ; Xie, Hua ; Ding, Jian ; Duan, Wenhu ; Xie, H (reprint author), Chinese Acad Sci, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai Inst Mat Med, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China.
刊名	MEDCHEMCOMM
	2015
英文摘要	Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive strategy for the treatment of cancer. Herein, we describe the design, synthesis, and biological evaluation of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors. Among the new derivatives, compound 3k exhibited high VEGFR-2 inhibitory potency in both enzymatic and VEGF-induced HUVEC cellular proliferation assays (IC50 = 0.5 and 9.8 nM, respectively). Kinase selectivity profiling revealed that 3k was a highly selective VEGFR-2 inhibitor. Moreover, 3k effectively inhibited angiogenesis in HUVEC tube formation assay.; Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive strategy for the treatment of cancer. Herein, we describe the design, synthesis, and biological evaluation of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors. Among the new derivatives, compound 3k exhibited high VEGFR-2 inhibitory potency in both enzymatic and VEGF-induced HUVEC cellular proliferation assays (IC50 = 0.5 and 9.8 nM, respectively). Kinase selectivity profiling revealed that 3k was a highly selective VEGFR-2 inhibitor. Moreover, 3k effectively inhibited angiogenesis in HUVEC tube formation assay.
内容类型	期刊论文
源URL	[http://ir.nwipb.ac.cn/handle/363003/5474]
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
推荐引用方式 GB/T 7714	Lv, Yongcong,Li, Mengyuan,Cao, Sufen,et al. Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors[J]. MEDCHEMCOMM,2015.
APA	Lv, Yongcong.,Li, Mengyuan.,Cao, Sufen.,Tong, Linjiang.,Peng, Ting.,...&Xie, H .(2015).Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors.MEDCHEMCOMM.
MLA	Lv, Yongcong,et al."Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors".MEDCHEMCOMM (2015).