| Project/Area Number |
23590005
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | Gifu University |
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Principal Investigator |
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| Project Period (FY) |
2011 – 2013
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| Project Status |
Completed (Fiscal Year 2013)
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| 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)
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| 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 |
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| 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.
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