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Preparation of various xylose derivatives as glycosaminoglycan biosynthesis inhibitor

Preparation of various xylose derivatives as glycosaminoglycan biosynthesis inhibitor
多种糖胺聚糖生物合成抑制剂木糖衍生物的制备
批准号:
23590005
负责人:
KOKETSU Mamoru
金额:
$3.33万
依托单位:
依托单位国家:
日本
项目类别:
Grant-in-Aid for Scientific Research (C)
财政年份:
2011
资助国家:
日本
项目状态:
已结题
起止时间:
2011 至 2013

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中文摘要
翻译
本研究考察了在木糖中引入疏水基团的各种木糖生物合成抑制剂的研究进展。目前的研究表明,含氟木糖苷类化合物是一种有效的血管内皮细胞形成的体外抑制剂。此外,还制备了各种木糖衍生物,用于开发木糖生物合成抑制剂。采用点击化学的方法合成了1,5-二取代-1,2,3-三氮唑衍生物。木糖硫脲类化合物与溴丙炔反应生成1,3-噻唑类化合物。与肼反应生成1,2,4-三氮唑衍生物。与叠氮化钠反应生成1,2,3,4-四唑类化合物。目前,这些木糖衍生物的GAG生物合成抑制能力正在进行中。
英文摘要
This study investigated the development of various GAG biosynthesis inhibitors introducing hydrophobic moieties into xylose.The current study demonstrates that fluoro-xylosides are effective inhibitors of endothelial tube formation in vitro using a matrigel based assay to simulate tumor-associated angiogenesis.In addition, various xylose derivatives were prepared for development of GAG biosynthesis inhibitor. 1,5-Disubstituted-1,2,3-triazole derivatives were synthesized by click chemistry using a ruthenium complex. The reaction of xylose thiourea derivatives with bromide propyne gave 1,3-thiazole derivatives. The reaction with hydrazine gave 1,2,4-triazole derivatives. And the reaction with sodium azide yielded 1,2,3,4-tetrazole derivatives, respectively. Currently, GAG biosynthesis inhibitory ability of these obtained xylose derivatives are carrying out.
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DOI: 10.1021/cb400132r
发表时间: 2013-05-01
期刊: ACS CHEMICAL BIOLOGY
影响因子: 4
作者: [Nguyen, Thao K. N., Tran, Vy M., Kuberan, Balagurunathan]
通讯作者: Kuberan, Balagurunathan
Development of high efficient synthesis method of selenium neucleosides and its application
  • 批准号:
    15K07856
  • 项目类别:
    Grant-in-Aid for Scientific Research (C)
  • 资助金额:
    $3.16万
  • 财政年份:
    2015
  • 负责人:
    KOKETSU Mamoru
  • 依托单位:
Preparation of novel beta-lactam derivatives using efficient leaving group
  • 批准号:
    20590005
  • 项目类别:
    Grant-in-Aid for Scientific Research (C)
  • 资助金额:
    $3.0万
  • 财政年份:
    2008
  • 负责人:
    KOKETSU Mamoru
  • 依托单位:
Development of heterocyclic compounds using various active species containing selenium
  • 批准号:
    17550099
  • 项目类别:
    Grant-in-Aid for Scientific Research (C)
  • 资助金额:
    $2.3万
  • 财政年份:
    2005
  • 负责人:
    KOKETSU Mamoru
  • 依托单位:
海外基金