Labeling of Proteins, Peptides, and Estrogens With Cyclopentadienyltricarbonylrhenium and Technetium
The conjugation of cyclopentadienyltricarbonylrhenium to molecules having an affinity for the estrogen receptor is described. A variety of derivatives were prepared using either an indirect labeling or a preformed chelate approach, and of the compounds synthesized, ((17$\beta$-estradiol-17$\alpha$-yl)-ethynylcyclopentadienyl) tricarbonylrhenium and its 11$\beta$-chloromethyl, ethyl and methoxy derivatives are attractive candidates for imaging estrogen receptors in vivo, having relative binding affinities (RBA's) for the estrogen receptor of 7.29%, 283%, 283% and 52.6%, respectively.
University of Illinois - Urbana-Champaign
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University of Illinois at Urbana-Champaign