CAS: 16732-57-3; Ethyl 5-Nitro-1H-Indole-2-Carboxylate

相似化合物

16730-20-4 71086-99-2 16792-45-3

上下游产品

CAS号73647-04-8 2-[2-(4-硝基苯基)亚肼... | CAS号2999-46-4 异氰基乙酸乙酯 | CAS号84459-32-5 2-溴-5-硝基苯甲醛 | CAS号63190-15-8 (Z)-ethyl 2-(p-... | CAS号617-35-6 丙酮酸乙酯 | CAS号636-99-7 4-硝基苯肼盐酸盐 | CAS号100-01-6 对硝基苯胺 | CAS号6146-52-7 5-硝基吲哚 | CAS号71086-99-2 5-氨基吲哚-2-甲酸乙酯 | CAS号5192-03-0 5-氨基吲哚 | CAS号101134-91-2 5-(1H-indole-2-... | CAS号152213-40-6 5-氨基-2-吲哚羧酸 | CAS号16730-20-4 5-硝基吲哚-2-甲酸 | CAS号152213-42-8 t-butyl 5-nitro... | CAS号199805-99-7 (5-nitro-1H-ind... | CAS号183384-45-4 Ethyl 3-bromo-5... | CAS号71056-57-0 1-甲基-5-硝基-1H-吲哚...

4-硝基苯肼置于polyphosphoric Acid体系中,用 乙醇 用作溶剂,化学反应 4.0H,反应生成5-硝基吲哚-2-羧酸乙酯
参考文献:作为新型nur77调节剂的5-(((8-甲氧基-2-甲基喹啉-4-基)氨基)-1H-吲哚-2-碳酰肼衍生物的设计,合成和生物学评估.
标题:作为新型nur77调节剂的5-(((8-甲氧基-2-甲基喹啉-4-基)氨基)-1H-吲哚-2-碳酰肼衍生物的设计,合成和生物学评估.
摘要:Nur77是治疗hcc等癌症的潜在靶标.在这里,我们详细介绍了新型的5-(((8-甲氧基-2-甲基喹啉-4-基)氨基)-1 H-吲哚-2-碳酰肼衍生物作为潜在的nur77调节剂系列.对目标化合物的抗增殖活性和nur77结合亲和力的研究导致发现了领先的候选药物(10G),它是一种非常好的nur77结合剂(k D = 3.58+/-0.16μm),对所有测试物质均具有广谱抗增殖活性肝癌细胞(ic 50 <2.0μm),对正常lo2细胞毒性低.10克可以上调nur77的表达并介导nur77的亚细胞定位以诱导肝癌细胞系的凋亡,这依赖于10G诱导nur77依赖性自噬和内质网应激作为凋亡的上游.此外,体内试验证实10G显着抑制异种移植肿瘤的生长.这些结果表明10G有潜力被开发为靶向nur77的新型抗肝癌药物.
Doi:10.1016/j.Ejmech.2020.112608

专利信息

专利号:US-7329760-B2
优先权日:2002-04-05
标题 :CC-1065 analog synthesis
发明人：ZHAO ROBERT YONGXIN; CHARI RAVI V J
权利人:IMMUNOGEN INC
摘要:Improved synthesis of seco(−)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2-dihydro-3H-benz(e)indole): n nand improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.

专利号:JP-2005522506-A
优先权日:2002-04-05
标 题 :Improved synthesis of CC-1065 related substances

专利号:ES-2286418-T3
优先权日:2002-04-05
标 题 :IMPROVED SYNTHESIS OF ANALOGS OF CC-1065.

专利号:PT-1492766-E
优先权日:2002-04-05
标题 :IMPROVED SYNTHESIS OF CC-1065 ANALOGS.

专利号:EP-1492766-A4
优先权日:2002-04-05
标 题 :IMPROVED SYNTHESIS OF CC-1065 ANALOGUE

专利号:US-8513241-B2
优先权日:2008-03-28
标题 :3,4-dihydro-2H-pyrazino[1,2-A]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
发明人：CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; SALOM BARBARA
权利人:CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; SALOM BARBARA; NERVIANO MEDICAL SCIENCES SRL
摘要:Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.