CAS: 183320-15-2; 2-((4-((3-Ethynylphenyl)Amino)-7-(2-Methoxyethoxy)Quinazolin-6-yl)Oxy)Ethyl Acetate
该化合物是一种复杂的有机化合物,具有独特的结构特征,含有一种五氯苯基,这是一种以其存在于各种生物活性化合物中而闻名的双环结构;一个苯基组的存在表明其在医药化学中的潜在应用,特别是在制药业中.甲基氧基化合物组可能提高溶性和生物利用率,而乙氧基化合物表明该化合物可能是影响其再活动性和稳定性的酯类.该化合物可能显示特定的生物活动,有可能在各种生物化学途径中起到抑制或调节作用.其合成和特征分析通常涉及标准的有机化学技术,其特性将通过光谱和染色学等方法加以评估.
- 英文名称2-((4-((3-Ethynylphenyl)Amino)-7-(2-Methoxyethoxy)Quinazolin-6-yl)Oxy)Ethyl Acetate
- 中文名称去甲基厄洛替尼乙酸酯
- IUPAC名称2-((4-((3-ethynylphenyl)amino)-7-(2-methoxyethoxy)quinazolin-6-yl)oxy)ethyl acetate
- 其它别名6-(2-Acetoxy-Ethoxy)-4-(3-Ethynyl-Phenylamino)-7-(2-Methoxy-Ethoxy)-Quinazoline; Desmethyl Erlotinib Acetate; 2-[[4-[(3-Ethynylphenyl)Amino]-7-(2-Methoxyethoxy)-6-Quinazolinyl]Oxy]Ethanol Acetate Ester; 2-[[4-[(3-Ethynylphenyl)Amino]-7-(2-Methoxyethoxy)-6-Quinazolinyl]Oxy]Ethanol 1-Acetate; 2-((4-((3-Ethynylphenyl)Amino)-7-(2-Methoxyethoxy)Quinazolin-6-yl)Oxy)Ethyl Acetate; Erlotinib 6-O-Desmethyl Acetate; Erlotinib Impurity ⅰ; 2-((4-((3-Ethynylphenyl)Amino)-7-(2-Methoxyethoxy)Quizolin-6-yl)Oxy)Ethylacetate
- CAS编号183320-15-2
- MFCD编号:MFCD09840372
- 分子式:C23H23N3O5分子量:421.45
- 产品CID: 942630
- 产品分类分析化学 → 标准品 → 药典标准品和杂质标准品
物理性质
MSDS等安全信息
合成工艺路线路线简述
📜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
海关参考信息
- 2901292000-乙炔
2902300000-甲苯
2905310000-1,2-乙二醇
2907210001-间苯二酚 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
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
