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  1. C100 医学部/医学系研究科
  2. C100a 雑誌掲載論文
  3. 学術雑誌

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
dfe6bd62-039a-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 170228_manuscript_MGMT_for_BMCL-D-16-02164_revised.pdf ファイル公開:2019/05/01 (796.9 kB)
Item type 学術雑誌論文 / Journal Article(1)
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
著者 Koyama, Hiroko

× Koyama, Hiroko

WEKO 73012

Koyama, Hiroko

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Ikenuma, Hiroshi

× Ikenuma, Hiroshi

WEKO 73013

Ikenuma, Hiroshi

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Toda, Hiroshi

× Toda, Hiroshi

WEKO 73014

Toda, Hiroshi

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Kondo, Goro

× Kondo, Goro

WEKO 73015

Kondo, Goro

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Hirano, Masaki

× Hirano, Masaki

WEKO 73016

Hirano, Masaki

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Kato, Masaya

× Kato, Masaya

WEKO 73017

Kato, Masaya

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Abe, Junichiro

× Abe, Junichiro

WEKO 73018

Abe, Junichiro

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Yamada, Takashi

× Yamada, Takashi

WEKO 73019

Yamada, Takashi

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Wakabayashi, Toshihiko

× Wakabayashi, Toshihiko

WEKO 73020

Wakabayashi, Toshihiko

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Ito, Kengo

× Ito, Kengo

WEKO 73021

Ito, Kengo

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Natsume, Atsushi

× Natsume, Atsushi

WEKO 73022

Natsume, Atsushi

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Suzuki, Masaaki

× Suzuki, Masaaki

WEKO 73023

Suzuki, Masaaki

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権利
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 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.
内容記述タイプ Abstract
出版者
出版者 Elsevier
言語
言語 eng
資源タイプ
資源タイプresource http://purl.org/coar/resource_type/c_6501
タイプ journal article
DOI
関連識別子
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 ISSN
収録物識別子 0960-894X
書誌情報 Bioorganic & Medicinal Chemistry Letters

巻 27, 号 9, p. 1892-1896, 発行日 2017-05
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
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