| Project/Area Number |
24790123
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Tokushima Bunri University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
TSUKAMOTO Ikuko 香川大学, 医学部 薬物生体情報学講座, 客員教授 (10183477)
IGARASHI Junsuke 香川大学, 医学部 自律機能生理学講座, 准教授 (20346638)
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| Project Period (FY) |
2012-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2015: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2014: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2013: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
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| Keywords | コアクロル / 血管新生促進活性 / 血管新生促進剤 / ２クロル炭素環オキセタノシンＡ / 血管新生促進作用 / 構造活性相関 / 核酸類縁体 / 2クロル炭素環オキセタノシンA / COA-Cl / S1P1受容体アゴニスト |
|---|
| Outline of Final Research Achievements |
Six novel carbocyclic oxetanocin A analogs (2-chloro-C.OXT-A; COA-Cl) with various hydroxymethylated or spiro-conjugated cyclobutane rings at the N9-position of the 2-chloropurine moiety were synthesized and evaluated using human umbilical vein endothelial cells. All prepared compounds showed good to moderate activity with angiogenic potency. Among these compounds, 100 μM cis-trans-2',3'-bis(hydroxymethyl)cyclobutyl derivative, trans-3'-hydroxymethylcyclobutyl analog, and 3',3'-bis(hydroxymethyl)cyclobutyl derivative had greater angiogenic activity, with relative tube areas of 3.43 ± 0.44, 3.32 ± 0.53, and 3.59 ± 0.83 (mean ± SD), respectively, which was comparable to COA-Cl (3.91 ± 0.78). These data may be important for further development of this class of compounds as potential tube formation agents.
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