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Preparation of various xylose derivatives as glycosaminoglycan biosynthesis inhibitor

Research Project

Project/Area Number 23590005
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Chemical pharmacy
Research InstitutionGifu University

Principal Investigator

KOKETSU Mamoru  岐阜大学, 工学部, 教授 (50178208)

Project Period (FY) 2011 – 2013
Project Status Completed (Fiscal Year 2013)
Budget Amount *help
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2013: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2012: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2011: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Keywordsグルコサミノグリカン / 阻害剤 / キシロース / クリックケミストリー / テトラゾール / トリアゾール / グリコサミノグリカン / 生合成阻害剤 / ヘテロ環
Research Abstract

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.

Report

(4 results)
  • 2013 Annual Research Report   Final Research Report ( PDF )
  • 2012 Research-status Report
  • 2011 Research-status Report
  • Research Products

    (3 results)

All 2013 2011 Other

All Journal Article (2 results) (of which Peer Reviewed: 2 results) Remarks (1 results)

  • [Journal Article] Dimerized Glycosaminoglycan Chains Increase FGF Signaling during Zebrafish Development2013

    • Author(s)
      Thao K. N. Nguyen, Vy M. Tran, Venkataswamy Sorna, Inger Eriksson, Akinori Kojima, Mamoru Koketsu, Duraikkannu Loganathan, Lena Kjellén, Richard I. Dorsky, Chi-Bin Chien, and Balagurunathan Kuberan
    • Journal Title

      ACS Chemical Biology

      Volume: 8 (5) Issue: 5 Pages: 939-948

    • DOI

      10.1021/cb400132r

    • Related Report
      2013 Annual Research Report 2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] Novel glycosaminoglycan biosynthetic inhibitors affect tumor-associated angiogenesis2011

    • Author(s)
      K. Raman, M. Ninomiya, T. K. N. Nguyen, Y. Tsuzuki, M. Koketsu, and B. Kuberan
    • Journal Title

      Biochem. Biophys. Res. Commun

      Volume: 404 Issue: 1 Pages: 86-89

    • DOI

      10.1016/j.bbrc.2010.11.069

    • Related Report
      2013 Final Research Report 2011 Research-status Report
    • Peer Reviewed
  • [Remarks]

    • URL

      http://www1.gifu-u.ac.jp/~ms2/flame_j.htm

    • Related Report
      2013 Final Research Report

URL: 

Published: 2011-08-05   Modified: 2019-07-29  

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