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Design, synthesis, and evaluation of cyclofenil derivatives for potential SPECT imaging agents.

Abstract
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.
AuthorsHua Zhu, Liliang Huang, Yuanqing Zhang, Xiaoping Xu, Yanhong Sun, Yu-Mei Shen
JournalJournal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry (J Biol Inorg Chem) Vol. 15 Issue 4 Pg. 591-9 (May 2010) ISSN: 1432-1327 [Electronic] Germany
PMID20195693 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Ligands
  • Octanols
  • Organotechnetium Compounds
  • Receptors, Estrogen
  • Water
  • Rhenium
  • Cyclofenil
Topics
  • Breast Neoplasms (diagnostic imaging, metabolism)
  • Cyclofenil (chemical synthesis, chemistry, metabolism)
  • Drug Design
  • Drug Stability
  • Humans
  • Ligands
  • Octanols (chemistry)
  • Organotechnetium Compounds (chemistry)
  • Receptors, Estrogen (metabolism)
  • Rhenium
  • Tomography, Emission-Computed, Single-Photon
  • Water (chemistry)

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