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Synthesis of PET probe O^6-[(3-[11C]methyl)benzyl]guanine by Pd^0-mediated rapid C-[11C]methylation toward imaging DNA repair protein O^6-methylguanine-DNA methyltransferase in glioblastoma
http://hdl.handle.net/2237/26868
http://hdl.handle.net/2237/26868dfe6bd62-039a-47f6-81dc-b0c20717aec5
| 名前 / ファイル | ライセンス | アクション |
|---|---|---|
170228_manuscript_MGMT_for_BMCL-D-16-02164_revised.pdf ファイル公開：2019/05/01 (796.9 kB)
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| Item type | 学術雑誌論文 / Journal Article(1) | |||||
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| 公開日 | 2017-08-02 | |||||
| タイトル | ||||||
| タイトル | Synthesis of PET probe O^6-[(3-[11C]methyl)benzyl]guanine by Pd^0-mediated rapid C-[11C]methylation toward imaging DNA repair protein O^6-methylguanine-DNA methyltransferase in glioblastoma | |||||
| 言語 | en | |||||
| 著者 |
Koyama, Hiroko
× Koyama, Hiroko× Ikenuma, Hiroshi× Toda, Hiroshi× Kondo, Goro× Hirano, Masaki× Kato, Masaya× Abe, Junichiro× Yamada, Takashi× Wakabayashi, Toshihiko× Ito, Kengo× Natsume, Atsushi× Suzuki, Masaaki |
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| アクセス権 | ||||||
| アクセス権 | open access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_abf2 | |||||
| 権利 | ||||||
| 言語 | en | |||||
| 権利情報 | © 2017. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ | |||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | O^6-Benzylguanine (O^6-BG) is a substrate of O^6-methylguanine-DNA methyltransferase (MGMT), which is involved in drug resistance of chemotherapy in the majority of glioblastoma multiform. For clinical diagnosis, it is hoped that the MGMT expression level could be determined by a noninvasive method to understand the detailed biological properties of MGMT-specific tumors. We synthesized 11C-labeled O^6-[(3-methyl)benzyl]guanine ([11C]mMeBG) as a positron emission tomography probe. Thus, a mixed amine-protected stannyl precursor, N9-(tert-butoxycarbonyl)-O^6-[3-(tributylstannyl)benzyl]-N2-(trifluoroacetyl)guanine, was subjected to rapid C-[11C]methylation under [11C]CH3I/[Pd2(dba)3]/P(o-CH3C6H4)3/CuCl/K2CO3 in NMP, followed by quick deprotection with LiOH/H2O, giving [11C]mMeBG with total radioactivity of 1.34 GBq and ≥99% radiochemical and chemical purities. | |||||
| 言語 | en | |||||
| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| 言語 | en | |||||
| 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 | |||||
| 出版タイプ | ||||||
| 出版タイプ | AM | |||||
| 出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||
| DOI | ||||||
| 関連タイプ | isVersionOf | |||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | https://doi.org/10.1016/j.bmcl.2017.03.045 | |||||
| ISSN | ||||||
| 収録物識別子タイプ | PISSN | |||||
| 収録物識別子 | 0960-894X | |||||
| 書誌情報 |
en : Bioorganic & Medicinal Chemistry Letters 巻 27, 号 9, p. 1892-1896, 発行日 2017-05 |
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| 著者版フラグ | ||||||
| 値 | author | |||||
| URI | ||||||
| 識別子 | http://hdl.handle.net/2237/26868 | |||||
| 識別子タイプ | HDL | |||||
