Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai, 201800, China.
J Biol Inorg Chem. 2010 May;15(4):591-9. doi: 10.1007/s00775-010-0627-0. Epub 2010 Mar 1.
To develop technetium- and rhenium-labeled nonsteroidal estrogen imaging agents for estrogen receptor (ER) positive breast tumors, two groups of rhenium and technetium cyclofenil derivatives were synthesized and characterized. The binding affinities of the rhenium complexes for ERs were determined. The tricarbonyl rhenium complex showed the highest binding affinity for ERs (81.2 for ERbeta, 16.5 for ERalpha). Tricarbonyl technetium cyclofenil complexes were obtained in high radiochemical purity and radiochemical yields. The results of studies of their octanol/water partition and in vitro stability are presented. These results demonstrate that these radiolabeled cyclofenil derivatives may be considered as potential breast cancer imaging agents.
为了开发用于雌激素受体 (ER) 阳性乳腺癌的锝和铼标记的非甾体雌激素成像剂，合成并表征了两组铼和锝环戊烯衍生物。测定了铼配合物与 ER 的结合亲和力。三羰基铼配合物对 ER 的结合亲和力最高（ERbeta 为 81.2，ERalpha 为 16.5）。获得了高放射化学纯度和放射化学产率的三羰基锝环戊烯配合物。给出了它们的辛醇/水分配系数和体外稳定性研究的结果。这些结果表明，这些放射性标记的环戊烯衍生物可被认为是潜在的乳腺癌成像剂。
