CAS: 398493-79-3; N-(2,6-Diethylphenyl)-3-(4-(4-Methylpiperazin-1-yl)Benzamido)-4,6-Dihydropyrrolo[3,4-C]Pyrazole-5(1H)-Carboxamide

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上下游产品

Ethyl 5-(2,6-Diethylphenylcarbamoyl)-3-[4-(4-Methylpiperazin-1-yl)Benzoylamino]-5,6-Dihydro-4H-Pyrrolo[3,4-C]Pyrazole-1-Carboxylate 850997-37-4
1-乙基氧基羰基-3-[4-(4-甲基-1-哌嗪)-苯甲酰基氨基]-5-Boc-4,6-二氢-吡咯并[3,4-C]吡唑 5-Tert-Butyl 1-Ethyl 3-{[4-(4-Methylpiperazin-1-yl)Benzoyl]Amino}-4,6-Dihydropyrrolo[3,4-C]Pyrazole-1,5-Dicarboxylate 761443-69-0
5-Boc-3-氨基-4,6-二氢吡咯并[3,4-C]吡唑-1-甲酸乙酯 3-Amino-4,6-Dihydro-Pyrrolo[3,4-C]Pyrazole-1,5-Dicarboxylic Acid 5-Tert-Butyl Ester 1-Ethyl Ester 398495-65-3

合成工艺路线路线简述

    📜3-氨基-5-叔丁氧羰基-吡咯并[3,4-C]吡唑置于盐酸,三乙胺,N,N-二异丙基乙胺体系中,用 四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷 作为反应溶剂,化学反应 62.0H,反应生成 N-(2,6-二乙基苯基)-4,6-二氢-3-[[4-(4-甲基-1-哌嗪基)苯甲酰基]氨基]吡咯并[3,4-C]吡唑-5(1H)-甲酰胺
    参考文献:Potent And Selective Aurora Inhibitors Identified By The Expansion Of A Novel Scaffold For Protein Kinase Inhibition
    标题:Potent And Selective Aurora Inhibitors Identified By The Expansion Of A Novel Scaffold For Protein Kinase Inhibition
    摘要:Potent And Selective Aurora Kinase Inhibitors Were Identified From The Combinatorial Expansion Of The 1,4,5,6-Tetrahydropyrrolo[3,4-C]Pyrazole Bi-Cycle,A Novel And Versatile Scaffold Designed To Target The Atp Pocket Of Protein Kinases. The Most Potent Compound Reported In This Study Had An Ic(50) Of 0.027 Microm In The Enzymatic Assay For Aur-A Inhibition And Ic(50)S Between 0.05 Microm And 0.5 Microm For The Inhibition Of Proliferation Of Different Tumor Cell Lines.
    DOI:10.1021/jm049076M

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    主要参考文献


    1: Polacchini A, Albani C, Baj G, Colliva A, Carpinelli P, Tongiorgi E. Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell death but surviving cells overproduce BDNF. Biol Open. 2016 Jun 2. pii: bio.016725. doi: 10.1242/bio.016725. [Epub ahead of print] doi: 10.1182/blood-2013-02-482356. Epub 2013 Aug 23. doi: 10.1038/onc.2011.314. Epub 2011 Jul 25.
    4: Tao Y, Zhang P, Frascogna V, Lecluse Y, Auperin A, Bourhis J, Deutsch E. Enhancement of radiation response by inhibition of Aurora-A kinase using siRNA or a selective Aurora kinase inhibitor PHA680632 in p53-deficient cancer cells. Br J Cancer. 2007 Dec 17;97(12):1664-72. Epub 2007 Nov 20.
    5: Soncini C, Carpinelli P, Gianellini L, Fancelli D, Vianello P, Rusconi L, Storici P, Zugnoni P, Pesenti E, Croci V, Ceruti R, Giorgini ML, Cappella P, Ballinari D, Sola F, Varasi M, Bravo R, Moll J. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res. 2006 Jul 1;12(13):4080-9. doi: 10.3324/haematol.2018.208280. Epub 2019 Apr 4.

    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:10.1182/blood-2013-02-482356
    摘要:Mazzera L, Lombardi G, Abeltino M, Ricca M, Donofrio G, Giuliani N, Cantoni AM, Corradi A, Bonati A, Lunghi P. Aurora and IKK kinases cooperatively interact to protect multiple myeloma cells from Apo2L/TRAIL. Blood. 2013 Oct 10;122(15):2641–53. doi: 10.1182/blood-2013-02-482356.
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