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1 PublicationRadiochemical synthesis and tissue distribution of Tc-99-labeled 7alpha-substituted estradiol complexes
Skaddan, M. B.; Wüst, F. R.; Jonson, S.; Syhre, R.; Welch, M. J.; Spies, H.; Katzenellenbogen, J. A.
Abstract
The diagnosis and staging of breast cancer could be improved by the development of radiopharmaceutical imaging agents that provide a noninvasive determination of the estrogen receptor (ER) status of tumor cells. Agents labeled with 99mTc would be especially valuable in this regards. In attempting to achieve this goal, we synthesized four 99mTc-labeled 7alpha-substituted estradiol complexes. One complex utilizes the "3+1" mixed ligand design to introduce the Tc metal, whereas the other three took advantage of the cyclopentadienyltricarbonylmetal (CpTM) design. The Tc moieties were attached to the 7alpha position of estradiol with a hexyl tether, a monoether tether, or a polyether tether. The corresponding rhenium compounds have binding affinities for the ER of 20-45% compared with estradiol. Radiochemical yields of the
Keywords: 99mTc; Estradiol; complexes; cyclopentadienyltricarbonyl; mixed ligand; 3+1
- Nuclear Medicine & Biology 27 (2000) 269-278
Permalink: https://www.hzdr.de/publications/Publ-3441