CAS: 190728-26-8; 6,7-Dimethoxy-4-(2-Nitrophenoxy)Quinoline (Cabozantinib Impurity)

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228559-85-1 190728-27-9 190728-24-6

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6,7-dimethoxy-4-chloroquinoline 2-hydroxynitrobenzene ethyl 6,7-dimethoxy-4-oxo-1,4-dihydro-3-quinolinecarboxylate 3,4-dimethoxyaniline

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参考文献:Synthesis And Structure-activity Relationship For New Series Of 4-Phenoxyquinoline Derivatives As Specific Inhibitors Of Platelet-Derived Growth Factor Receptor Tyrosine Kinase
标题:Synthesis And Structure-activity Relationship For New Series Of 4-Phenoxyquinoline Derivatives As Specific Inhibitors Of Platelet-Derived Growth Factor Receptor Tyrosine Kinase
摘要:We Discovered A New Series Of 4-Phenoxyquinoline Derivatives As Potent And Selective Inhibitors Of The Platelet-Derived Growth Factor Receptor (Pdgfr) Tyrosine Kinase. We Researched The Highly Potent And Selective Inhibitors On The Basis Of Both Pdgfr And Epidermal Growth Factor Receptor (Egfr) Inhibitory Activity. First,We Found A Compound,Ki6783 (1),Which Inhibited Pdgfr Autophosphorylation At 0.13 Mum,But It Did Not Inhibit Egfr Autophosphorylation At 100 Mum. After Extensive Explorations,We Found The Two Desired Compounds,Ki6896 (2) And Ki6945 (3),Which Are Substituted By Benzoyl And Benzamide At The 4-Position Of The Phenoxy Group On 4-Phenoxyquinoline,Respectively. These Inhibitory Activities Were 0.31 And 0.050 Mum,Respectively,But Neither Of Them Inhibited Egfr Autophosphorylation At 100 M. We Further Investigated The Profile Of Both Compounds Toward Various Tyrosine And Serine/threonine Kinases. The Three Compounds Specifically Inhibited Pdgfr Rather Than The Other Kinases. (C) 2003 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2003.08.020