CAS: 443797-96-4; 4-((5-Amino-1-(2,6-Difluorobenzoyl)-1H-1,2,4-Triazol-3-yl)Amino)Benzenesulfonamide

该化合物是一种化学化合物,其结构复杂,包括一个磺酰胺组和一个三氮基.该化合物通常具有极地溶剂的高溶性和其他潜在生物活动等特性,因此对制药研究感兴趣,特别是抗微生物剂或抗硫剂的研制.二氟苯并基组的存在可能加强其亲性与生物活动.此外,氨基和磺酰胺的功能有助于其与生物目标的再活动及潜在互动.该化合物的分子结构表明,它可能参与氢的结合和其他分子间相互作用,这对生物系统的效率至关重要.

结构式图片

上下游产品

CAS号172935-91-0 2,6-二氟苯甲酰肼 | CAS号79463-77-7 N-氰基羰亚胺二苯基酯 | CAS号63-74-1 磺胺 | CAS号700805-72-7 N-[4-(aminosulf... | CAS号443799-31-3 4-(5-amino-1H-[... | CAS号18063-02-0 2,6-二氟苯甲酰氯 | CAS号51908-29-3 4-异硫氰基苯磺酰胺

合成工艺路线路线简述

    Phenyl-N'-Cyano-N-(4-Sulfamoylphenyl)Carbamimidate置于吡啶,肼体系中,用 四氢呋喃 作为反应溶剂,化学反应 8.0H,反应生成 Aurora激酶
    参考文献:1-Acyl-1H-[1,2,4]Triazole-3,5-Diamine Analogues As Novel And Potent Anticancer Cyclin-Dependent Kinase Inhibitors: Synthesis And Evaluation Of Biological Activities
    标题:1-Acyl-1H-[1,2,4]Triazole-3,5-Diamine Analogues As Novel And Potent Anticancer Cyclin-Dependent Kinase Inhibitors: Synthesis And Evaluation Of Biological Activities
    摘要:A Series Of 1-Acyl-1H-[1,2,4]Triazole-3,5-Diamine Analogues Were Synthesized As Cyclin-Dependent Kinase (Cdk) Inhibitors. These Compounds Showed Potent And Selective Cdk1 And Cdk2 Inhibitory Activities And Inhibited In Vitro Cellular Proliferation In Various Human Tumor Cells. Representative Compound 3B Demonstrated In Vivo Efficacy In A Human Melanoma A375 Xenograft Model In Nude Mice.
    DOI:10.1021/jm050267E

    海关参考信息

    专利信息


    专利号:US-11285169-B2
    优先权日:2013-03-13
    标题 :Methods for modulating chemotherapeutic cytotoxicity
    发明人:ROBERTS DAVID D; SOTO PANTOJA DAVID R
    权利人:US HEALTH
    摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.
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    主要参考文献


    1: Matsuhashi A, Ohno T, Kimura M, Hara A, Saio M, Nagano A, Kawai G, Saitou M, Takigami I, Yamada K, Okano Y, Shimizu K. Growth suppression and mitotic defect induced by JNJ-7706621, an inhibitor of cyclin-dependent kinases and aurora kinases. Curr Cancer Drug Targets. 2012 Jul;12(6):625-39. doi: 10.1042/BJ20110592. doi: 10.1016/j.ijpharm.2010.03.018. Epub 2010 Mar 11. Epub 2006 May 6.

    合成参考文献


    参考文献:10.1042/bj20110592
    摘要:Pflug A, de Oliveira TM, Bossemeyer D, Engh RA. Mutants of protein kinase A that mimic the ATP-binding site of Aurora kinase. Biochem J. 2011 Nov 15;440(1):85–93. doi: 10.1042/bj20110592.
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