Knowledge Management System of Northwest Institute of Plateau Biology, CAS
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. | |
2015 | |
发表期刊 | MEDCHEMCOMM
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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. |
文献类型 | 期刊论文 |
条目标识符 | http://210.75.249.4/handle/363003/47816 |
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 | 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). |
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