CAS: 228559-41-9; 1-(2,4-Difluorophenyl)-3-(4-((6,7-Dimethoxyquinolin-4-yl)Oxy)-2-Fluorophenyl)Urea

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2,4-diflurophenylis°Cyanate 4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2-fluoroaniline 6,7-dimethoxy-4-chloroquinoline 2-amino-4,5-dimethoxyacetophenone

2'-氨基-4',5'-二甲氧基苯乙酮置于sodium Methylate,氯化铵,锌,三氯氧磷体系中,用 甲醇,乙二醇二甲醚,氯苯,甲苯 用作溶剂,化学反应 23.67H,反应生成Ki 8751; N-(2,4-二氟苯基)-N'-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-2-氟苯基]脲
参考文献:Novel Potent Orally Active Selective Vegfr-2 Tyrosine Kinase Inhibitors: Synthesis,Structure−activity Relationships,And Antitumor Activities Of N-Phenyl-N'-{4-(4-Quinolyloxy)Phenyl}Ureas
标题:Novel Potent Orally Active Selective Vegfr-2 Tyrosine Kinase Inhibitors: Synthesis,Structure−activity Relationships,And Antitumor Activities Of N-Phenyl-N'-{4-(4-Quinolyloxy)Phenyl}Ureas
摘要:N-Phenyl-N'-{4-(4-Quinolyloxy)Phenyl}Ureas Were Found To Be A Novel Class Of Potent Inhibitors For The Vascular Endothelial Growth Factor Receptor 2 (Vegfr-2) Tyrosine Kinase Through Synthetic Modifications Of A Lead Compound And Structure-Activity Relationship Studies. A Representative Compound 6Ab,Termed Ki8751,Inhibited Vegfr-2 Phosphorylation At An Ic50 Value Of 0.90 Nm,And Also Inhibited The Pdgfr Family Members Such As Pdgfr(X And C-Kit At 67 Nm And 40 Nm,Respectively. However,6Ab Did Not Have Any Inhibitory Activity Against Other Kinases Such As Egfr,Hgfr,Insulinr And Others Even At 10000 Nm. 6Ab Suppressed The Growth Of The Vegf-Stimulated Human Umbilical Vein Endothelial Cell (Huvec) On A Nanomolar Level. 6Ab Showed Significant Antitumor Activity Against Five Human Tumor Xenografts Such As Gl07 (Glioma),St-4 (Stomach Carcinoma),Lc6 (Lung Carcinoma),Dld-1 (Colon Carcinoma) And A375 (Melanoma) In Nude Mice And Also Showed Complete Tumor Growth Inhibition With The Lc-6 Xenograft In Nude Rats Following Oral Administration Once A Day For 14 Days At 5 Mg/kg Without Any Body Weight Loss.
Doi:10.1021/jm030427R