Synthesis of new carbon-11 labeled cyclofenil derivatives for PET imaging of breast cancer estrogen receptors.

Abstract

Carbon-11 labeled cyclofenil derivatives, [(11)C]methyl-2-{4-[bis(4-hydroxyphenyl)methylene]cyclohexyl}acetate ([(11)C]16a), [(11)C]methyl-4-[bis(4-hydroxyphenyl)methylene]cyclohexanecarboxylate ([(11)C]16b), [(11)C]methyl-2-{3-[bis(4-hydroxyphenyl)methylene]cyclohexyl}acetate ([(11)C]18a), and [(11)C]methyl-3-[bis(4-hydroxyphenyl)methylene]cyclohexanecarboxylate ([(11)C]18b), have been synthesized as new potential PET agents for imaging breast cancer estrogen receptors. The target tracers were prepared by O-[(11)C]methylation of their corresponding precursors using [(11)C]CH(3)OTf and isolated by a simplified SPE purification procedure in 35-50% radiochemical yields decay corrected to EOB, 15-20 min overall synthesis time, and 74-111 GBq/micromol specific activity at EOS.

• Authors: Mingzhang Gao, Min Wang, Bruce H Mock, Kathy D Miller, George W Sledge, Gary D Hutchins, Qi-Huang Zheng
• Journal: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (Appl Radiat Isot) Vol. 66 Issue 4 Pg. 523-9 (Apr 2008) ISSN: 0969-8043 [Print] England
• PMID: 18155914 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Carbon Radioisotopes
• Radiopharmaceuticals
• Receptors, Estrogen
• Cyclofenil

Topics

• Breast Neoplasms (diagnostic imaging, metabolism)
• Carbon Radioisotopes (chemistry)
• Cyclofenil (analogs & derivatives, chemical synthesis)
• Female
• Humans
• Magnetic Resonance Spectroscopy
• Positron-Emission Tomography (methods)
• Radiopharmaceuticals (chemical synthesis)
• Receptors, Estrogen (analysis, biosynthesis)