Journal
BIOCONJUGATE CHEMISTRY
Volume 16, Issue 2, Pages 255-264Publisher
AMER CHEMICAL SOC
DOI: 10.1021/bc049770g
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Funding
- NCI NIH HHS [1 R24 CA83060, 1 P30 CA91842, 5R37 CA25836, R24 CA863071] Funding Source: Medline
- NCRR NIH HHS [RR 01575, 1 S10 RR104444] Funding Source: Medline
- NIGMS NIH HHS [GM 27029] Funding Source: Medline
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Cyclopentadienyl tricarbonylmetal (CpTM, M = Re, Tc-94m) complexes, some based on a typical nonsteroidal estrogen, were prepared with the aim of developing technetium- and rhenium-labeled imaging agents for estrogen receptor (ER) positive breast tumors. CpT[Tc-94m] compounds with simple cyclopentadienyl substituents were first synthesized using a modified double ligand transfer reaction. The in vivo biodistribution of one of these CPT[Tc-94m] complexes was determined by tissue dissection and microPET imaging. Novel C-ring substituted analogues of cyclofenil, a nonsteroidal compound known to bind the ER, were also prepared, and their ER binding was measured. Because of their low ER affinity, however, labeling and imaging studies of these compounds were not pursued. It is notable that the highest ER binding analogue, a CpTRe cyclofenil derivative, could be synthesized from the corresponding ferrocenyl cyclofenil analogue by the double ligand transfer reaction. This further demonstrates the versatility of the double ligand transfer reaction and indicates that the synthesis of technetium and rhenium radiolabeled agents for breast tumor imaging and therapy is also likely to be successful.
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