CAS: 910297-51-7; N-(2-Chloro-6-Methylphenyl)-2-((2-Methyl-6-(Piperazin-1-yl)Pyrimidin-4-yl)Amino)Thiazole-5-Carboxamide

该化合物是一种合成有机化合物,其结构复杂,包括三硝酸盐环,一个碳boxamide组,以及多种芳香和热循环成分.该化合物的特点是氯代苯组和一种管状苯,有助于其潜在的生物活动.硫酸和环的存在表明可能与生物目标发生相互作用,使其对药用化学,特别是药物开发感兴趣.其分子结构表明,该化合物可能具有诸如有机溶液溶性,各种条件下的稳定性和特定受体约束性成分等特性.该化合物的设计可能旨在加强治疗应用的功效和选择性,有可能在诸如肿瘤学或...

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CAS号110-85-0 哌嗪 | CAS号302964-08-5 N-(2-氯-6-甲基苯基)-... | CAS号910297-62-0 达沙替尼羧酸乙酯

合成工艺路线路线简述

  • 302964-08-5 = 910297-51-7
    反应条件:1.1 Reagents: Diisopropylethylamine Solvents: 1-Butanol; 16 H,110 °C1.2 Solvents: Methanol,Water; 1 H,60 °C
    标题:Discovery Of Siais178 As An Effective Bcr-Abl Degrader By Recruiting Von Hippel-Lindau (Vhl) E3 Ubiquitin Ligase
    作者:Zhao,Quanju; Ren,Chaowei; Liu,Linyi; Chen,Jinju; Shao,Yubao; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2019 卷标:62(20) 页码:9281-9298]

    1159977-13-5 = 910297-51-7
    反应条件:1.1 Reagents: Trifluoroacetic Acid Solvents: Dichloromethane; 16 H,Rt1.2 Reagents: Sodium Bicarbonate Solvents: Dichloromethane,Water; Rt
    标题:Assessing Different E3 Ligases For Small Molecule Induced Protein Ubiquitination And Degradation
    作者:Ottis,Philipp; Toure,Momar; Cromm,Philipp M.; Ko,Eunhwa; Gustafson,Jeffrey L.; Et Al
    参考文献:Acs Chemical Biology 日期:2017 卷标:12(10) 页码:2570-2578]

    302964-08-5 = 910297-51-7
    反应条件:1.1 Reagents: Diisopropylethylamine Solvents: 1,4-Dioxane; Overnight,80 °C
    标题:Global Protac Toolbox For Degrading Bcr-Abl Overcomes Drug-Resistant Mutants And Adverse Effects
    作者:Yang,Yiqing; Gao,Hongying; Sun,Xiuyun; Sun,Yonghui; Qiu,Yueping; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2020 卷标:63(15) 页码:8567-8583]

    302964-08-5 = 910297-51-7
    反应条件:1.1 Reagents: Diisopropylethylamine Solvents: 1,4-Dioxane; 4 H,100 °C
    标题:Controlling Cellular Distribution Of Drugs With Permeability Modifying Moieties
    作者:Richardson,Paul L.; Marin,Violeta L.; Koeniger,Stormy L.; Baranczak,Aleksandra; Wilsbacher,Julie L.; Et Al
    参考文献:Medchemcomm 日期:2019 卷标:10(6) 页码:974-984]

    1159977-13-5 = 910297-51-7
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water; 3 H,55 - 60 °C
    标题:A Convenient New And Efficient Commercial Synthetic Route For Dasatinib (Sprycel)
    作者:Suresh,Garbapu; Nadh,Ratnakaram Venkata; Srinivasu,Navuluri; Yennity,Durgaprasad
    参考文献:Synthetic Communications 日期:2017 卷标:47(17) 页码:1610-1621]

    1159977-13-5 = 910297-51-7
    反应条件:1.1 Reagents: Trifluoroacetic Acid Solvents: Dichloromethane; 4 H,Rt
    标题:Synthesis And Biological Evaluation Of Novel Dasatinib Analogues As Potent Ddr1 And Ddr2 Kinase Inhibitors
    作者:Liu,Lu; Hussain,Muzammal; Luo,Jinfeng; Duan,Anna; Chen,Chaonan; Et Al
    参考文献:Chemical Biology & Drug Design 日期:2017 卷标:89(3) 页码:420-427]

    302964-08-5 = 910297-51-7
    反应条件:1.1 Reagents: Diisopropylethylamine Solvents: 1,4-Dioxane; Overnight,Reflux
    标题:Synthesis And Biological Evaluation Of A Fluorine-18 Derivative Of Dasatinib
    作者:Veach,Darren R.; Namavari,Mohammad; Pillarsetty,Nagavarakishore; Santos,Elmer B.; Beresten-Kochetkov,Tatiana; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2007 卷标:50(23) 页码:5853-5857]

    302964-08-5 = 910297-51-7
    反应条件:1.1 Reagents: Diisopropylethylamine Solvents: 1,4-Dioxane; Overnight,Reflux
    标题:Azo-Protac: Novel Light-Controlled Small-Molecule Tool For Protein Knockdown
    作者:Jin,Yu-Hui; Lu,Meng-Chen; Wang,Yan; Shan,Wen-Xin; Wang,Xuan-Yu; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2020 卷标:63(9) 页码:4644-4654
📜N-(2-氯-6-甲基苯基)-2-[(6-氯-2-甲基-4-嘧啶基)氨基]-5-噻唑甲酰胺置于三乙胺,三氟乙酸体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 16.0H,反应生成 N-(2-氯-6-甲基苯基)-2-{[2-甲基-6-(1-哌嗪基)-4-嘧啶基]氨基}-1,3-噻唑-5-甲酰胺
参考文献:新型达沙替尼类似物作为有效的ddr1和ddr2激酶抑制剂的合成和生物学评估.
标题:新型达沙替尼类似物作为有效的ddr1和ddr2激酶抑制剂的合成和生物学评估.
摘要:设计并合成了作为ddr1和ddr2抑制剂的新型达沙替尼类似物.筛选合成的化合物的ddr1和ddr2激酶抑制作用以及癌细胞增殖抑制活性.一些化合物对ddr1和ddr2均显示出有效的抑制活性,并且在低纳摩尔范围内对k562细胞系具有抗癌活性.特别是,化合物3J对两个ddr的抑制力均明显优于亲代达沙替尼,并且对k562细胞系也具有有效的抑制活性(ddr1的ic50值为2.26 +/-0.46 Nm,Ddr2的ic50值为7.04 +/-2.90 Nm,0.125对于k562细胞系,为+/-0.017 Nm.本文受版权保护.版权所有.
DOI:10.1111/cbdd.12863

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主要参考文献

参考标题:Design And Synthesis Of Novel Dasatinib Analogues
作者:G. Buchappa,K. Durgaprasad,B. Suneelkumar,P. Baby Rani,K. Ravi Babu,A.K.S. Bhujanga Rao,P. Aparna
摘要:Design, Synthesis, Characterization And In Vitro Biological Assay Of A Series Of Novel Carboxylic Acid And Amino Acid Analogs Of Dasatinib (1) As Anticancer Agents Are Reported. Some Of The Synthesized Analogs Were Identified As Potent Src/abl Kinase Inhibitors With Greater Antiproliferative Activity Against K652 And T315I Cancer Cell Lines. The Synthetic Process Involves Condensation Of N-(2-Chloro-6-Methylphenyl)-2-[[6-[4(-1-Pipearazinyl]-2-Methyl-4-Pyrimidinyl]Amino]-5-Thiazolecarboxamide With Carboxylic Acids In The Presence Of Dicyclohexylcarbodiimide And Oxyma In Organic Solvent Medium. Compounds Were Characterized And Tested For Anticancer Activity On Leukemia Cancer Cell Lines K562 And Baf3/t315. Analogues Of Lactic Acid, Mandalic Acid, Leucine And Proline Have Shown Promising Antiproliferative Activity Compared To Dasatinib.

合成参考文献

合成方法参考DOI号:10.1039/c8md00412a
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