CAS: 183320-15-2; 2-((4-((3-Ethynylphenyl)Amino)-7-(2-Methoxyethoxy)Quinazolin-6-yl)Oxy)Ethyl Acetate

4-苄氧基-3-羟基苯甲酸乙酯置于硫酸,Palladium On Activated Charcoal,氢气,硝酸,甲酸铵,Potassium Carbonate,溶剂黄146,三氯氧磷体系中,用 乙酸乙酯,N,N-二甲基甲酰胺,异丙醇 用作溶剂,化学反应生成去甲基厄洛替尼乙酸酯
参考文献:新型七甲胺花青染料-埃罗替尼偶联物作为抗肿瘤剂的设计,合成和生物学评估.
标题:新型七甲胺花青染料-埃罗替尼偶联物作为抗肿瘤剂的设计,合成和生物学评估.
摘要:表皮生长因子受体酪氨酸激酶(egfr-Tk)已被证明是治疗具有特定基因突变的非小细胞肺癌(nsclc)的靶标.但是,Egfr-Tk抑制剂(egfr-Tkis)需要进入癌细胞,然后与酪氨酸激酶受体的活性位点竞争性相互作用,以抑制下游信号通路来抑制肿瘤的增殖.在这项研究中,为了提高egfr-Tki的肿瘤细胞靶向能力,将egfr-Tki厄洛替尼与靶向癌细胞的七甲亚胺花青染料缀合,以形成17种新型厄洛替尼-染料缀合物.在体外评估了缀合物针对癌细胞生长和egfr-Tk抑制的肿瘤靶向特性的效率.结果显示,大多数厄洛替尼-染料偶联物比母体药物厄洛替尼对a549,H460,H1299和mda-Mb-231细胞系表现出更强的抑制作用.同时,代表性化合物对人正常乳腺上皮mcf-10A细胞表现出弱的细胞毒性.此外,共轭ce17也表现出〜14倍高的egfr-Tk抑制活性(ic 50 = 0.124μm)厄洛替尼相比(ic
Doi:10.1016/j.Bmcl.2020.127557

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

专利号:CN-103483275-B
优先权日:2012-11-19
标题:Coupling compound of NSAID anti-inflammatory analgesic drug and EGFR kinase inhibitor and its synthesis method and application