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Utilization of [11C]phosgene for radiosynthesis of N-(2-{3-[3,5-bis(trifluoromethyl)] phenyl[11C]ure2;ido}ethyl)glycyrrhetinamide, an inhibitory agent for proteasome and kinase in tumors
https://repo.qst.go.jp/records/46335
https://repo.qst.go.jp/records/46335f798d764-071d-45e4-b69c-a985d8df049e
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2012-06-05 | |||||
| タイトル | ||||||
| タイトル | Utilization of [11C]phosgene for radiosynthesis of N-(2-{3-[3,5-bis(trifluoromethyl)] phenyl[11C]ure2;ido}ethyl)glycyrrhetinamide, an inhibitory agent for proteasome and kinase in tumors | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Asakawa, Chiharu
× Asakawa, Chiharu× Ogawa, Masanao× Fujinaga, Masayuki× Kumata, Katsushi× Xie, Lin× Yamasaki, Tomoteru× Yui, Joji× Fukumura, Toshimitsu× Zhang, Ming-Rong× 浅川 千春× 小川 政直× 藤永 雅之× 熊田 勝志× 謝 琳× 山崎 友照× 由井 譲二× 福村 利光× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | N-(2-{3-[3,5-Bis(trifluoromethyl)]phenylureido}ethyl)glycyrrhetinamide (2), an ureido-substituted derivative of glycyrrhetinic acid (1), has been reported to display potent inhibitory activity for proteasome and kinase, which are overexpressed in tumors. In this study, we labeled this unsymmetrical urea 2 using [11C]phosgene ([11C]COCl2) as a labeling agent with the expectation that [11C]2 could become a positron emission tomography ligand for the imaging of proteasome and kinase in tumors. The strategy for the radiosynthesis of [11C]2 was to react hydrochloride of 3,5-bis(trifluoromethyl)aniline (4HCl) with [11C]COCl2 to possibly give isocyanate [11C]6, followed by the reaction of [11C]6 with N-(2-aminoethyl) glycyrrhetinamide (3). |
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| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 22, 号 11, p. 3594-3597, 発行日 2012-04 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0960-894X | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | org/10.1016/j.bmcl.2012.04.049 | |||||
