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化学学报
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化学学报 ›› 2011, Vol. 69 ›› Issue (10): 1197-1204. 上一篇    下一篇

研究论文

4-取代环芬尼类化合物的合成及标记

朱华1,2,4, 林建国1, 沈玉梅*,2,3   

  1. (1江苏省原子医学研究所 卫生部核医学重点实验室 江苏省分子核医学重点实验室 无锡 214063)
    (2中国科学院上海应用物理研究所 物理生物学研究室 上海 201800)
    (3上海交通大学系统生物医学研究院 系统生物医学教育部重点实验室 上海 200240)
    (4中国科学院研究生院 北京 100049)
  • 投稿日期:2010-10-15 修回日期:2010-12-07 发布日期:2011-01-20
  • 通讯作者: 沈玉梅 E-mail:yumeishen@sjtu.edu.cn
  • 基金资助:

    卫生部核医学重点实验室, 江苏省分子核医学重点实验室 开放课题基金;中国科学院“百人计划”;国家自然科学基金

Synthesis and Radio-labeling of 4-Substituted Cyclofenil

Zhu Hua1,2,4,Lin Jianguo1,Shen Yumei*,2,3   

  1. (1 Key Laboratory of Nuclear Medicine Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063)
    (2 Laboratory of Physical Biology, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800)
    (3 Key Laboratory of Systems Biomedicine of Ministry of Education, Shanghai Center for Systems Biomedicine, Shanghai Jiao Tong University, Shanghai 200240)
    (4 Graduate School of the Chinese Academy of Sciences, Beijing 100049)
  • Received:2010-10-15 Revised:2010-12-07 Published:2011-01-20
  • Contact: Yu-Mei Shen E-mail:yumeishen@sjtu.edu.cn

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以Cyclofenil为原料, 合成得到一系列氟乙氧基衍生物. 通过受体结合实验, 筛选得到一个对雌激素受体(ER)具有高特异性和高相对亲和力(RBA)的化合物Penta-Cyclofenil-FEt. 通过实验的优化设计, 合成得到相应的氟标记前体, 产物通过IR, UV, 1H NMR, 19F NMR或ESI-HRMS进行了表征. 在冷试条件下, 得到了冷氟取代参比化合物. 在热试验条件下, 得到F-18标记产物. 此类非甾体雌激素受体分子探针的合成, 为PET (positron emission tomography)显像雌激素受体β从而评估乳腺癌的恶化程度奠定了基础.

关键词: 环芬尼, 氟乙基, 乳腺癌, 亲和力, PET显像

Starting from cyclofenil, a serial of cyclofenil-FEt derivatives were prepared. Generally speaking pentacyclofenil-FEt has greater relative binding affinity (RBA) to estradiol receptors than that of estradiol. The precursor compounds were synthesized for potential radioactive imaging agents, and their structures were characterized by ultraviolet, infrared, 1H NMR, 19F NMR, and ESI-HRMS techniques. The non- radioactive/radioactive compounds were synthesized. The study provides a useful assessment of the stage of the breast cancer by imaging ERβ with the PET (positron emission tomography) imaging.

Key words: cyclofenil, fluoroethyl, breast cancer, binding affinity, PET imaging