CAS: 896705-16-1; N-(2-(Dimethylamino)Ethyl)-12-Oxo-12H-Benzo[g]Pyrido[2,1-B]Quinazoline-4-Carboxamide
- 英文名称N-(2-(Dimethylamino)Ethyl)-12-Oxo-12H-Benzo[g]Pyrido[2,1-B]Quinazoline-4-Carboxamide
- 中文名称N-[2-(二甲基氨基)乙基]-12-氧代-12H-苯并[g]吡啶并[2,1-b]喹唑啉-4-甲酰胺
- IUPAC名称N-(2-(dimethylamino)ethyl)-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide
- CAS编号896705-16-1
- MFCD编号:MFCD27225377
- EINECS号:809-833-1
- 分子式:C21H20N4O2分子量:360.42
- 产品CID: 1918410
- 产品分类有机原料 → 有机杂环化合物 → 吡啶并嘧啶类
物理性质
MSDS等安全信息
欧盟法规
C&L通报上下游产品
2-chloronicotinic acid 2-Amino-3-naphthoic acid N,N-dimethylethylenediamine 12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxylic acid合成工艺路线路线简述
- 108-00-9 + 63127-04-8 = 896705-16-1
反应条件:1.1 Reagents: Diisopropylethylamine,O-(Benzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Tetrafluoroborate Solvents: Dimethylformamide; 15 Min,Rt1.2 16 H,Rt1.3 Reagents: Water; Cooled
标题:Design,Synthesis,And Structure-Activity Relationships Of Pyridoquinazolinecarboxamides As Rna Polymerase I Inhibitors
作者:Colis,Laureen; Ernst,Glen; Sanders,Sara; Liu,Hester; Sirajuddin,Paul; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:2014 卷标:57(11) 页码:4950-4961
📜3-氨基-2-萘甲酸置于盐酸,O-(Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Tetrafluoroborate,N,N-二异丙基乙胺体系中,用 乙醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 82.25H,反应生成 N-[2-(二甲基氨基)乙基]-12-氧代-12H-苯并[g]吡啶并[2,1-B]喹唑啉-4-甲酰胺
参考文献: Compounds Which Inhibit Rna Polymerase,Compositions Including Such Compounds,And Their Use[fr] Composés Qui Inhibent L'Arn Polymérase,Compositions Comprenant De Tels Composés,Et Leur Utilisation
标题: Compounds Which Inhibit Rna Polymerase,Compositions Including Such Compounds,And Their Use[fr] Composés Qui Inhibent L'Arn Polymérase,Compositions Comprenant De Tels Composés,Et Leur Utilisation
摘要:Rna聚合酶i(pol I)是专门用于转录47S核糖体rna前体的聚合酶,随后将其加工成成熟的5.8S,18S和28S核糖体rna,并在核仁中组装成核糖体.pol I活性在人类癌症中常常失调.基于引物分子bmh-21的发现,合成了一系列吡啶喹唑啉羧酰胺作为pol I的抑制剂和rpa194的破坏激活剂,Rpa194是pol I的大催化亚基蛋白.本发明确定了一组生物活性化合物,包括纯化的立体异构体,它们能够有效地导致rpa194的降解,这些化合物在一个严格受限制的化学空间中发挥作用.还提供了包括这些化合物的药物组合物及其在癌症和其他与pol I相关疾病中的用途.
海关参考信息
- 2902200000-苯
2902902000-精萘
2912110000-甲醛
2921211000-乙二胺 - 💡 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-2023160018-A1
优先权日:2020-04-16
标 题 :Crybetab2 predicts poor breast cancer outcome and sensitizes tumors to nucleolin and cdk inhibition
发明人：MERINO VANESSA FERREIRA; POMPER MARTIN; SUKUMAR SARASWATI
权利人:UNIV JOHNS HOPKINS
摘要:CKYPB2 induces EMT, sternness, protein synthesis and cell cycle progression through regulation of nucleolin, con-tributing to an increase in tumor growth and metastasis. CKYPB2 can be used as a prognostic marker in African American women with TNBC. CKYPB2 can further select patients with TNBC and ER positive tumors that will likely benefit from inhibitors of ribosomal RNA synthesis, CDK4 and nucleolin.
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品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Peltonen K, Colis L, Liu H, Jäämaa S, Zhang Z, Af Hällström T, Moore HM, Sirajuddin P, Laiho M. Small Molecule BMH-Compounds That Inhibit RNA Polymerase I and Cause Nucleolar Stress. Mol Cancer Ther. 2014 Nov;13(11):2537-46. doi: 10.1158/1535-7163.MCT-14-0256. Epub 2014 Oct 2.
2: Colis L, Peltonen K, Sirajuddin P, Liu H, Sanders S, Ernst G, Barrow JC, Laiho M. DNA intercalator BMH-21 inhibits RNA polymerase I independent of DNA damage response. Oncotarget. 2014 Jun 30;5(12):4361-9.
3: Colis L, Ernst G, Sanders S, Liu H, Sirajuddin P, Peltonen K, DePasquale M, Barrow JC, Laiho M. Design, synthesis, and structure-activity relationships of pyridoquinazolinecarboxamides as RNA polymerase I inhibitors. J Med Chem. 2014 Jun 12;57(11):4950-61. doi: 10.1021/jm5004842. Epub 2014 May 30.
合成参考文献
参考文献:10.1124/mol.119.115964
摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
参考文献:10.1002/pros.23909
摘要:Low JY, Sirajuddin P, Moubarek M, Agarwal S, Rege A, Guner G, Liu H, Yang Z, De Marzo AM, Bieberich C, Laiho M. Effective targeting of RNA polymerase I in treatment-resistant prostate cancer. Prostate. 2019 Dec;79(16):1837–51.
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