CAS: 66622-47-7; 2-(3-Isobutylphenyl)Propanoic Acid

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CAS号124-38-9 二氧化碳 | CAS号859828-57-2 methyl 2-(3-iso... | CAS号621-37-4 3-羟基苯乙酸 | CAS号42058-59-3 3-羟基苯乙酸甲酯

📜3-羟基苯乙酸置于氢氧化钾,四(三苯基膦)钯,硫酸,Sodium Hydride,N,N-二异丙基乙胺体系中,用 四氢呋喃,甲醇,二氯甲烷 作为反应溶剂,化学反应 25.67H,反应生成 布洛芬杂质a
参考文献:2-Arylpropionic Cxc Chemokine Receptor 1 (Cxcr1) Ligands As Novel Noncompetitive Cxcl8 Inhibitors
标题:2-Arylpropionic Cxc Chemokine Receptor 1 (Cxcr1) Ligands As Novel Noncompetitive Cxcl8 Inhibitors
摘要:The Cxc Chemokine Cxcl8/il-8 Plays A Major Role In The Activation And Recruitment Of Polymorphonuclear (Pmn) Cells At Inflammatory Sites. Cxcl8 Activates Pmns By Binding The Seven-Transmembrane (7-Tm) G-Protein-Coupled Receptors Cxc Chemokine Receptor 1 (Cxcr1) And Cxc Chemokine Receptor 2 (Cxcr2). (R)-Ketoprofen (1) Was Previously Reported To Be A Potent And Specific Noncompetitive Inhibitor Of Cxcl8-Induced Human Pmns Chemotaxis. We Report Here Molecular Modeling Studies Showing A Putative Interaction Site Of 1 In The Tm Region Of Cxcr1. The Binding Model Was Confirmed By Alanine Scanning Mutagenesis And Photoaffinity Labeling Experiments. The Molecular Model Driven Medicinal Chemistry Optimization Of 1 Led To A New Class Of Potent And Specific Inhibitors Of Cxcl8 Biological Activity. Among These,Repertaxin (13) Was Selected As A Clinical Candidate Drug For Prevention Of Post-Ischemia Reperfusion Injury.
DOI:10.1021/jm049082I

专利信息

专利号:US-9452220-B2
优先权日:2014-12-23
标 题 :Coupling compounds of NSAID anti-inflammatory and analgesic drugs and EGFR kinase inhibitors, synthesis methods and applications thereof
发明人：ZHANG YANMEI; DING KE; LIAO JINXI; WANG YICAN; CHEN PANYU
权利人:GUANGZHOU INST BIOMED & HEALTH
摘要:The present invention discloses coupling compounds of a structure as shown in Formula I, II or III formed by connecting NSAID anti-inflammatory and analgesic drugs and EGFR inhibitors by ester bonds or pharmaceutically acceptable salts or stereoisomers thereof or prodrug molecules thereof: n n n n n n n n n n n n where R is a NSAID anti-inflammatory and analgesic drug. In the present invention, the coupling compounds obtained by coupling NSAID anti-inflammatory and analgesic drugs with EGFR inhibitors have excellent therapeutic effects of tumors and provide new drugs for clinic treatment options.

专利号:US-2016175453-A1
优先权日:2014-12-23
标题 :Coupling compounds of nsaid anti-inflammatory and analgesic drugs and egfr kinase inhibitors, synthesis methods and applications thereof