『徳島大学 教育・研究者情報データベース (EDB)』---[学外] /
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EID=130702EID:130702, Map:0, LastModified:2006年1月10日(火) 10:11:09, Operator:[近江 千代子], Avail:TRUE, Censor:0, Owner:[宇都 義浩], Read:継承, Write:継承, Delete:継承.
種別 (必須): 国際会議 [継承]
言語 (必須): 英語 [継承]
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組織 (推奨): 1.徳島大学.工学部.生物工学科.生物機能工学講座 [継承]
著者 (必須): 1.堀 均
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[継承]
2.永澤 秀子 (岐阜薬科大学/->個人[紺世 秀子])
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3.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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4. (英) Hiraoka Masamitsu (日) 平岡 正光 (読)
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5. (英) Goto Keiko (日) 後藤 恵子 (読)
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6. (英) Nakashima Hitomi (日) 中嶌 瞳 (読)
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7.後藤 了
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8. (英) Masunaga Shin-ichiro (日) (読)
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題名 (必須): (英) Design, synthesis, and pharmacokinetics of hypoxic tumor-targeting boron carriers  (日)    [継承]
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要約 (任意): (英) Purpose: The presence of hypoxic tumor cells is also associated with resistance to boron neutron capture therapy (BNCT). To accomplish the effective boron carrier for BNCT, we have recently developed 2-nitroimidazole-sodium borocaptate-10B (BSH) conjugates, TX-2016, 2017, 2018, 2041, 2042, and 2060, that is, hybrids that have both hypoxic tumor cell g-ray-sensitizing unit, 2-nitroimidazoles, and thermal neutron-sensitizing unit, BSH [1]. Furthermore, In this communication, to improve the hypoxia-targating character, we report the design, synthesis, and pharmacokinetics of hypoxic cytotoxin-hybrid boron carriers, TX-2091, 2095, 2097, 2100, 2124 and 2125, having hypoxic cytotoxin moiety, such as 2-quinoxalinecarbonitrile-1,4-di-N-oxide (TX-402) and tirapazamine (TPZ), and BSH via some carbon chain linker as a pharmacokinetic controlling unit. Result: TX-2016, 2017, and 2018: tertamethylammonium salts of alkyl sulfides of BSH. TX-2041, 2042 and 2060: sodium salts of an alkyl sulfide or a dialkyl sulfonium derivatives of BSH. They were synthesized from their corresponding haloacetylcarbamoyl-2-nitroimidazoles[2] and BSH. To synthesize hypoxic cytotoxin conjugate, 3-clorinated hypoxic cytotoxin (TX-402 or TPZ) was condensed with ethyl-, propyl-, or hexyl-alcoholamine to obtain the corresponding hydroxyalkylamino derivatives. They were treated with bromoacetyl isocyanate followed by disodium (2-cyanoethyl)-thio-undecahydro-closo-dodecaborate(2-) to yield cyanoethyl sulfonium compounds, TX-2095, 2100, 2110, 2124, and 2125. Among the 2-nitroimidazole conjugates, TX-2041 has the most favorable pharmacokinetic characteristics with higher tumor affinity of 10B during neutron beam irradiation. In addition, TX-2041 showed a significantly higher radiosensitizating effect with reactor thermal neutron beams than that of BSH. Cyanoethyl sulufonium derivative, TX-2060 showed better tumor affinity of 10B and more cytotoxicity after irradiation with reactor thermal neutron beams than that of TX-2041. Furthermore, TX-2100 achieved significantly higher tumor affinity than 2-nitoroimidazoles, TX-2041 and 2060, and also showed cytotoxicity comparable to TX-2060. In conclusion, these hypoxic tumor trageting cytotoxin-hybrid 10B-carriers , such as TX-2100, with the potential tumor affinty of10B, are expected to have clinical applications as promising boron carriers for use in BNCT.  (日)    [継承]
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誌名 (必須): (英) IMEBORON12 (日) 第12回国際ホウ素化学会議 (読)
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都市 (必須): 仙台 (Sendai/[日本国]) [継承]
年月日 (必須): 西暦 2005年 9月 15日 (平成 17年 9月 15日) [継承]
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標準的な表示

和文冊子 ● Hitoshi Hori, Hideko Nagasawa, Yoshihiro Uto, Masamitsu Hiraoka, Keiko Goto, Hitomi Nakashima, Satoru GOTO and Shin-ichiro Masunaga : Design, synthesis, and pharmacokinetics of hypoxic tumor-targeting boron carriers, IMEBORON12, (巻), (号), (頁), Sendai, Sep. 2005.
欧文冊子 ● Hitoshi Hori, Hideko Nagasawa, Yoshihiro Uto, Masamitsu Hiraoka, Keiko Goto, Hitomi Nakashima, Satoru GOTO and Shin-ichiro Masunaga : Design, synthesis, and pharmacokinetics of hypoxic tumor-targeting boron carriers, IMEBORON12, (巻), (号), (頁), Sendai, Sep. 2005.

関連情報

Number of session users = 3, LA = 0.70, Max(EID) = 361887, Max(EOID) = 968255.