NWIPB OpenIR
Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors
Lv, Yongcong1; Li, Mengyuan2,3; Cao, Sufen1,4; Tong, Linjiang2; Peng, Ting2; Wei, Lixin3; Xie, Hua2; Ding, Jian2; Duan, Wenhu1; 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
Source PublicationMEDCHEMCOMM
Volume6Issue:7Pages:1375-1380
SubtypeArticle
AbstractVascular 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.
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS KeywordENDOTHELIAL GROWTH-FACTOR ; RENAL-CELL CARCINOMA ; FACTOR RECEPTOR ; KINASE INHIBITORS ; ANGIOGENESIS ; CANCER ; DISEASE
Indexed BySCI
Language英语
WOS Research AreaBiochemistry & Molecular Biology ; Pharmacology & Pharmacy
WOS SubjectBiochemistry & Molecular Biology ; Chemistry, Medicinal
WOS IDWOS:000357786200020
Citation statistics
Cited Times:7[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://210.75.249.4/handle/363003/5474
Collection中国科学院西北高原生物研究所
Corresponding AuthorXie, 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.
Affiliation1.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
3.Chinese Acad Sci, Northwest Inst Plateau Biol, Qinghai 81008, Peoples R China
4.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China
Recommended Citation
GB/T 7714
Lv, Yongcong,Li, Mengyuan,Cao, Sufen,et al. Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors[J]. MEDCHEMCOMM,2015,6(7):1375-1380.
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,6(7),1375-1380.
MLA Lv, Yongcong,et al."Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors".MEDCHEMCOMM 6.7(2015):1375-1380.
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