Radiosynthesis of 10-(2-[18F]fluoroethoxy)-20(S)-camptothecin as a potential positron emission tomography tracer for the imaging of topoisomerase I in cancers

被引：1
作者：
Liu, Zhen-feng [1 ]
Wang, Guo-lin [1 ]
Dong, Meng-jie [1 ]
Jin, Jian-wen [2 ]
Li, Jia-jun [2 ]
Zhang, Qian [2 ]
Zhao, Kui [1 ]
Yang, Shu-ye [1 ]
Lin, Xiang-tong [3 ]
机构：
[1] Zhejiang Univ, Affiliated Hosp 1, Coll Med, PET Ctr, Hangzhou 310003, Zhejiang, Peoples R China
[2] Fudan Univ, Sch Pharm, Dept Med Chem, Shanghai 201203, Peoples R China
[3] Fudan Univ, Huashan Hosp, Dept Nucl Med, Shanghai 200400, Peoples R China
来源：
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2014年 / 299卷 / 03期
关键词：
10-(2-[F-18]fluoroethoxy)-20(S)-camptothecin; 2-[F-18]fluoroethyl bromide; PET tracer; F-18; Topoisomerase I; AUTOMATED SYNTHESIS; CAMPTOTHECIN; PET; BIODISTRIBUTION; EXPRESSION; MOLECULES; ANALOGS; AGENTS; F-18; MICE;
D O I：
10.1007/s10967-013-2862-7
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
摘要：
The preparation of 10-(2-[F-18]fluoroethoxy)-20(S)-camptothecin, a potential positron emission tomography tracer for the imaging of topoisomerase I in cancers, is described. 10-(2-[F-18]Fluoroethoxy)-20(S)-camptothecin was synthesized by the [F-18]fluoroalkylation of the corresponding hydroxy precursor molecule with 2-[F-18]fluoroethyl bromide ([F-18]FEtBr) in dimethylsulfoxide (DMSO) at 55 degrees C for 20 min; this was followed by purification using high performance liquid chromatography (HPLC) with a total preparation time of 60 min. The overall radiochemical yield was approximately 5.4-12 % (uncorrected), and the radiochemical purity was above 96 %.
引用
收藏
页码：1509 / 1515
页数：7
相关论文
共 29 条
[1]   RETRACTED: Radiosynthesis of 18F-labeled N-desmethyl-loperamide analogues for prospective molecular imaging radiotracers (Retracted Article) [J].
Bao, Xiaofeng ;
Liu, Duliang .
TETRAHEDRON LETTERS, 2013, 54 (11) :1412-1415
[2]   Automated synthesis and purification of [18F]bromofluoromethane at high specific radioactivity [J].
Bergman, J ;
Eskola, O ;
Lehikoinen, P ;
Solin, O .
APPLIED RADIATION AND ISOTOPES, 2001, 54 (06) :927-933
[3]   Preparation and biological evaluation of 2-amino-6-[18F]fluoro-9-(4-hydroxy-3-hydroxy-methylbutyl) purine (6-[18F]FPCV) as a novel PET probe for imaging HSV1-tk reporter gene expression [J].
Cai, Hancheng ;
Yin, Duanzhi ;
Zhang, Lan ;
Yang, Xlaofeng ;
Xu, Xiaoyan ;
Liu, Weiguo ;
Zheng, Xuesheng ;
Zhang, Hong ;
Wang, Jing ;
Xu, Yuhong ;
Cheng, Dengfeng ;
Zheng, Mingqiang ;
Han, Yanjiang ;
Wu, Mingxing ;
Wang, Yongxian .
NUCLEAR MEDICINE AND BIOLOGY, 2007, 34 (06) :717-725
[4]   A meta-analysis of the value of fluorodeoxyglucose-PET/PET-CT in the evaluation of fever of unknown origin [J].
Dong, Meng-jie ;
Zhao, Kui ;
Liu, Zhen-feng ;
Wang, Guo-lin ;
Yang, Shu-ye ;
Zhou, Guo-jun .
EUROPEAN JOURNAL OF RADIOLOGY, 2011, 80 (03) :834-844
[5]   Radiosynthesis of [11C]Vandetanib and [11C]chloro-Vandetanib as new potential PET agents for imaging of VEGFR in cancer [J].
Gao, Mingzhang ;
Lola, Christian M. ;
Wang, Min ;
Miller, Kathy D. ;
Sledge, George W. ;
Zheng, Qi-Huang .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (11) :3222-3226
[6]  
Hara T, 2002, J NUCL MED, V43, P187
[7]   Preliminary in vivo and ex vivo evaluation of the 5-HT2A imaging probe [18F]MH.MZ [J].
Herth, Matthias M. ;
Piel, Markus ;
Debus, Fabian ;
Schmitt, Ulrich ;
Lueddens, Hartmut ;
Roesch, Frank .
NUCLEAR MEDICINE AND BIOLOGY, 2009, 36 (04) :447-454
[8]  
HSIANG YH, 1985, J BIOL CHEM, V260, P4873
[9]   Topoisomerase I expression in tumors as a biological marker for CPT-11 chemosensitivity in patients with colorectal cancer [J].
Ikeguchi, Masahide ;
Arai, Yosuke ;
Maeta, Yoshihiko ;
Ashida, Keigo ;
Katano, Kuniyuki ;
Wakatsuki, Toshiro .
SURGERY TODAY, 2011, 41 (09) :1196-1199
[10]   Fluorine-18 and medical imaging: Radiopharmaceuticals for positron emission tomography [J].
Le Bars, Didier .
JOURNAL OF FLUORINE CHEMISTRY, 2006, 127 (11) :1488-1493
123