CAS: 20876-36-2; 5-Aminoindolin-2-One

上下游产品

2-吲哚酮 2-Oxoindole 59-48-3
5-硝基-1,3-二氢-2H-吲哚-2-酮 5-Nitrooxindole 20870-79-5
5-氨基靛红 5-Aminoisatin 42816-53-5
靛红 Indole-2,3-Dione 91-56-5
5-硝基靛红 5-Nitroisatin 611-09-6

5-硝基-1,3-二氢-2H-吲哚-2-酮置于铁粉,氯化铵体系中,用 乙醇,水 用作溶剂,化学反应 1.2H,以99%的收率获得5-氨基-1,3-二氢吲哚-2-酮
参考文献:作为有效brd4抑制剂的吲哚-2-酮衍生物的设计,合成和生物学评估.
标题:作为有效brd4抑制剂的吲哚-2-酮衍生物的设计,合成和生物学评估.
摘要:Bromodomain蛋白4(brd4)在转录调控中起着至关重要的作用,被认为是治疗癌症的可行药物靶标.在本文中,我们通过支架跳跃药物设计设计并合成了一系列吲哚-2-酮衍生物.大多数化合物在癌细胞系中显示出有效的brd4抑制活性和抗增殖活性.特别是,化合物12J表现出出色的brd4抑制活性(bd1 Ic 50 = 19 Nm,Bd2 Ic 50 = 28 Nm)和ic 50的抗增殖能力在ht-29和hl-60细胞中,其分别为4.75μm和1.35μm的值.此外,对接研究表明,靠近kac区和wpf架子的疏水口袋对化合物的活性至关重要.化合物12J可以阻止ht-29细胞进入g1期的细胞周期进程,并降低c-Myc的表达.此外,化合物12J表现出有利的口服药代动力学性质.所有结果表明,化合物12J是有效的brd4抑制剂,仅具有治疗结肠癌的潜力.
Doi:10.1016/j.Ejmech.2020.112780

专利信息

专利号:US-8933227-B2
优先权日:2009-08-14
标题 :Selective synthesis of functionalized pyrimidines
发明人：LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN
权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT
摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.

专利号:WO-9948868-A9
优先权日:1998-03-26
标 题 :Heterocyclic classes of compounds for the modulating tyrosine protein kinase
发明人：FONG ANNIE; HANNAH ALISON; HARRIS G DAVIS; HIRTH PETER; HUBBARD STEVEN R; LANGECKER PETER; LIANG CONGXIN; MCMAHON GERALD; MOHAMMADI MOOSA; SCHLESSINGER JOSEPH; SHAWVER LAURA K; SUN LI; TANG PENG C; ULLRICH AXEL
权利人:SUGEN INC; UNIV NEW YORK; MAX PLANCK INST FUR BIOCHEMIE; FONG ANNIE; HANNAH ALISON; HARRIS G DAVIS; HIRTH PETER; HUBBARD STEVEN R; LANGECKER PETER; LIANG CONGXIN; MCMAHON GERALD; MOHAMMADI MOOSA; SCHLESSINGER JOSEPH; SHAWVER LAURA K; SUN LI; TANG PENG C; ULLRICH AXEL
摘要:The invention relates to certain indolinone-based and pyrazolylamide-based compounds, their method of synthesis, and combinatorial libraries consisting of the compounds. The invention also relates to methods of modulating the function of protein kinases using these compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.

专利号:US-6514981-B1
优先权日:1998-04-02
标题:Methods of modulating tyrosine protein kinase function with indolinone compounds
发明人：TANG PENG CHO; SUN LI
权利人:SUGEN INC
摘要:The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.

专利号:CA-2718858-A1
优先权日:2008-03-20
标题:Selective synthesis of substituted pyrimidines

专利号:US-9351974-B2
优先权日:2011-11-10
标题 :Substituted pteridinones for the treatment of cancer
发明人：JIN MEIZHONG; KADALBAJOO MRIDULA; LI AN-HU; MULVIHILL MARK J; SIU KAM W; STEINIG ARNO G; WANG JING
权利人:OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: n npharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.

专利号:US-6680335-B2
优先权日:1998-09-28
标题 :Methods of modulating protein tyrosine kinase function with substituted indolinone compounds
发明人：TANG PENG CHO
权利人:SUGEN INC
摘要:The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.