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学科主题: 临床医学
题名:
Synthesis and evaluation of fluoroethyl cyclofenil analogs: Models for potential estrogen receptor imaging agent
作者: Zhu, Hua2; Yang, Zhi2; Lin, Jian-Guo3; Luo, Shi-Neng3; Shen, Yu-Mei1
关键词: Cyclofenil ; Estrogen receptor ; Relative binding affinity ; Fluorine-18
刊名: JOURNAL OF FLUORINE CHEMISTRY
发表日期: 2012-07-01
DOI: 10.1016/j.jfluchem.2012.04.005
卷: 139, 页:46-52
收录类别: SCI ; IC ; CCR
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Inorganic & Nuclear ; Chemistry, Organic
研究领域[WOS]: Chemistry
关键词[WOS]: POSITRON-EMISSION-TOMOGRAPHY ; BREAST-CANCER ; FLUORINE-18-LABELED ESTROGENS ; ESTRADIOL DERIVATIVES ; STRUCTURE-AFFINITY ; MAMMARY-TUMORS ; BETA ; LIGANDS ; TRANSCRIPTION ; PROSTATE
英文摘要:

Cyclofenil analogs (2a-2f) and their fluorine-containing derivatives (3a-3f) were synthesized and evaluated as candidate ligands for positron emission tomography (PET) imaging of estrogen receptors. Most of them show relatively high binding affinities comparable with estradiol (E-2). (4-Fluoroethoxyphenyl)-(4-hydroxyphenyl) methylenecyclopentane (3a) showed both the highest binding affinity for ERs (88.6 for ER beta, 13.8 for ER alpha) and highest beta/alpha ratio (beta/alpha for 6.4-fold). The radioactive compound [F-18]3a was prepared via displacement of the corresponding mesylate precursor 4 with [F-18]fluoride (F-18: beta(+): 96.7%, T-1/2 = 109.8 min). The biodistribution studies in immature female SD rats demonstrated that the uptake in the uterus and ovaries were 1.358 +/- 0.089% ID/g, 1.439 +/- 0.214% ID/g, respectively, both of the ratios of uterus/blood and ovaries/blood was less than 2:1. Micro-PET imaging of immature female SD rats has also been reported. (C) 2012 Elsevier B.V. All rights reserved.

语种: 英语
所属项目编号: 81071250 ; 81071198 ; 81172082 ; 21001055 ; 2011ZX09501-001-05 ; 200983
项目资助者: Natural Science Foundation of China ; National Key New Drug Creation and Development Program ; Ministry of Health Key Laboratory of Nuclear Medicine
WOS记录号: WOS:000305204100006
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/62844
Appears in Collections:北京大学临床肿瘤学院_核医学科_期刊论文

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作者单位: 1.Shanghai Jiao Tong Univ, Key Lab Syst Biomed, Minist Educ, Shanghai Ctr Syst Biomed, Shanghai 200240, Peoples R China
2.Peking Univ, Canc Hosp & Inst, Dept Nucl Med, Minist Educ,Key Lab Carcinogenesis & Translat Res, Beijing 100142, Peoples R China
3.Jiangsu Inst Nucl Med, Jiangsu Key Lab Mol Nucl Med, Minist Hlth, Key Lab Nucl Med, Wuxi 214063, Jiangsu, Peoples R China

Recommended Citation:
Zhu, Hua,Yang, Zhi,Lin, Jian-Guo,et al. Synthesis and evaluation of fluoroethyl cyclofenil analogs: Models for potential estrogen receptor imaging agent[J]. JOURNAL OF FLUORINE CHEMISTRY,2012,139:46-52.
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