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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (05): 715-723. 上一篇    下一篇

研究论文

新型聚乙二醇(PEG)-Cyclofenil雌激素受体分子β探针的合成

杨光1,2，朱华1,2，沈玉梅*,1,3   

  1. (1中国科学院上海应用物理研究所 上海 201800)
    (2中国科学院研究生院 北京 100049)
    (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)
  • 收稿日期:2010-10-03 修回日期:2010-12-21 发布日期:2010-12-30
  • 通讯作者: 沈玉梅 E-mail:yumeishen@sjtu.edu.cn

Synthesis of Novel Polyethylene Glycol (PEG)-Cyclofenil as Molecu-lar Probe of Estrogen Receptor β

Yang Guang1,2 Zhu Hua1,2 Shen Yumei*,1,3   

  1. (1 Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800)
    (2 Graduate School of the Chinese Academy of Sciences, Beijing 100049)
    (3 Key Laboratory of Systems Biomedicine, Ministry of Education, Shanghai Center for Systems Biomedicine, Shanghai Jiao Tong University, Shanghai 200240)
  • Received:2010-10-03 Revised:2010-12-21 Published:2010-12-30
  • Contact: Yu-Mei Shen E-mail:yumeishen@sjtu.edu.cn

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基于Cyclofenil对雌激素β受体的选择性结合能力, 完成了用于乳腺癌单光子发射计算机断层成像(SPECT)显像的新型聚乙二醇(PEG)-cyclofenil分子探针前体的合成, 并用99mTc对该前体进行放射化学标记. Cyclofenil的PEG修饰作为整个合成过程的关键步骤, 反应快速高效, 产率高达98%, 可在30 min内反应完全. 整个合成过程在较温和的反应条件下完成, 具有高产率、速度快的特点, 该实验为放射性标记试验及micro-SPECT成像奠定了良好的基础.

关键词: 环芬尼, 雌激素β受体, SPECT显像, 乳腺癌

New polyethylene glycol (PEG)-cyclofenil analogues based on its good affinity to estrogen receptor β, containing tridentate ligand chelating system, were synthesized as molecular probe precursors for single-photon emission computed tomography (SPECT) imaging of breast cancer. The precursors were radiolabeled with 99mTc successfully. The key step in the process was the preparation of PEG-substituted cyclofenil and the reaction was clear with high yield (98%) and rapid reaction rate (com-pleted within 30 min). Each step of the whole process was performed with relatively high yield under mild conditions. The exploration is extremely valuable for the radiolabeled experiment and micro-SPECT imag-ing study.

Key words: cyclofenil, estrogen receptor β, SPECT imaging, breast cancer