| ○種別 (必須): | □ | 学術論文 (審査論文)
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| ○言語 (必須): | □ | 英語
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| ○招待 (推奨): |
| ○審査 (推奨): | □ | Peer Review
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| ○カテゴリ (推奨): | □ | 研究
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| ○共著種別 (推奨): |
| ○学究種別 (推奨): |
| ○組織 (推奨): | 1. | 生命情報工学 (2006年4月1日〜2016年3月31日)
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| ○著者 (必須): | 1. | (英) Nakae Takashi (日) (読)
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| 2. | 宇都 義浩 ([徳島大学.大学院社会産業理工学研究部.生物資源産業学域.応用生命系.応用生物資源学分野]/[徳島大学.生物資源産業学部.生物資源産業学科.応用生命講座])
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| 3. | (英) Tanaka Motoko (日) (読)
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| 4. | (英) Shibata Haruna (日) (読)
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| 5. | 中田 栄司
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| 6. | 富永 正英 ([徳島大学.大学院医歯薬学研究部.保健科学域.保健科学部門.放射線科学系.医用画像解析学]/[徳島大学.医学部.保健学科.放射線技術科学専攻.診療放射線技術学講座])
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| 7. | 前澤 博
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| 8. | (英) Hashimoto Toshihiro (日) (読)
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| 9. | (英) Kirk L. Kenneth (日) (読)
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| 10. | 永澤 秀子 (岐阜薬科大学/->個人[紺世 秀子])
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| 11. | 堀 均
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| ○題名 (必須): | □ | (英) Design, synthesis, and radiosensitizing activities of sugar-hybrid hypoxic cell radiosensitizers (日)
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| ○副題 (任意): |
| ○要約 (任意): | □ | (英) We have designed sugar-hybrid TX-1877 derivatives conjugated with sugar moieties including β-glucose (β-Glc), β-galactose (β-Gal), α-mannose (α-Man) and N-acetyl-β-galactosamine (β-GalNAc). Compound 1 (TX-1877) was glycosylated with appropriate peracetylated sugars using BF3-OEt2 to give acetylated sugar-hybrids, 5 (TX-2244), 6 (TX-2245), 7 (TX-2246), and 10 (TX-2243). Removal of the acetyl groups afforded the sugar-hybrids having free hydroxyl groups, 11 (TX-2141), 12 (TX-2218), 13 (TX-2217) and 14 (TX-2068). We evaluated their radiosensitizing activities by an in vitro radiosensitization assay. All free hydroxyl hybrids have lower enhancement ratio (ER) values (ER 1.43) and lower n-octanol/water partition coefficient (Poct) values (Poct < 1.00 × 10-2) than does 1 (TX-1877, ER = 1.75, Poct: 5.60 × 10-2). All acetylated hybrids have similar Poct values (3.55 × 10-2 1.05 × 10-1) to 1 (TX-1877) and have improved ER values (ER 1.47) compared to the hybrids having free hydroxyl groups. Among these, 5 (TX-2244) is the most active radiosensitizer (ER = 2.30). We found a good correlation (r = 0.866) between the magnitude of Poct (logPoct) and the ER value of 5 (TX-2244), 6 (TX-2245), 7 (TX-2246), 10 (TX-2243) and 1 (TX-1877), suggesting that increasing the hydrophobicity is reflected in increased in vitro radiosensitizing activity. In the present study, we have succeeded in producing sugar-hybrid hypoxic cell radiosensitizers that have an increased radiosensitizing activity that does not depend on increased hydrophobicity. (日)
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| ○キーワード (推奨): | 1. | (英) Hypoxic cell radiosensitizers (日) (読)
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| 2. | (英) Sugar-hybrids (日) (読)
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| 3. | (英) Electronic states (日) (読)
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| 4. | (英) Hydrophobicity (日) (読)
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| ○発行所 (推奨): | □ | Elsevier Science
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| ○誌名 (必須): | □ | Bioorganic & Medicinal Chemistry ([Elsevier Science])
(pISSN: 0968-0896, eISSN: 1464-3391)
| ○ISSN (任意): | □ | 1464-3391
ISSN: 0968-0896
(pISSN: 0968-0896, eISSN: 1464-3391) Title: Bioorganic & medicinal chemistryTitle(ISO): Bioorg. Med. Chem.Publisher: Elsevier Ltd. (NLM Catalog)
(Scopus)
(CrossRef)
(Scopus information is found. [need login]) | [継承] |
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| ○巻 (必須): | □ | 16
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| ○号 (必須): | □ | 2
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| ○頁 (必須): | □ | 675 682
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| ○都市 (任意): |
| ○年月日 (必須): | □ | 西暦 2008年 1月 15日 (平成 20年 1月 15日)
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| ○URL (任意): |
| ○DOI (任意): | □ | 10.1016/j.bmc.2007.10.035 (→Scopusで検索)
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| ○PMID (任意): | □ | 18029186 (→Scopusで検索)
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| ○NAID (任意): |
| ○WOS (任意): | □ | 000253581500007
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| ○備考 (任意): | 1. | (英) Article.Affiliation: Department of Life System, Institute of Technology and Science, Graduate School, The University of Tokushima, Minamijosanjimacho-2, Tokushima 770-8506, Japan. (日)
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| 2. | (英) Article.PublicationTypeList.PublicationType: Journal Article (日)
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| 3. | (英) Article.PublicationTypeList.PublicationType: Research Support, N.I.H., Intramural (日)
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| 4. | (英) Article.PublicationTypeList.PublicationType: Research Support, Non-U.S. Gov't (日)
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