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Fluorine-18 click radiosynthesis and preclinical evaluation of a new 18F-labeled folic acid derivative.
Journal article

Fluorine-18 click radiosynthesis and preclinical evaluation of a new 18F-labeled folic acid derivative.

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  • 2008-12-05
Published in:
  • Bioconjugate chemistry. - 2008
Animals
Carrier Proteins
Drug Evaluation, Preclinical
Fluorine Radioisotopes
Folate Receptors, GPI-Anchored
Folic Acid
Humans
KB Cells
Male
Mice
Microsomes, Liver
Positron-Emission Tomography
Radiochemistry
Radiopharmaceuticals
Receptors, Cell Surface
Staining and Labeling
Stereoisomerism
Substrate Specificity
Tissue Distribution
English The folate receptor (FR) is highly expressed on most epithelial cancer cells, while normal cells show only restricted expression of FR. As a result, the FR is an ideal target for receptor-based molecular imaging and therapy of cancer and has become a promising target in oncology. To date, several folate-based chemotherapeutics and imaging probes such as radiopharmaceuticals for single photon emission computed tomography (SPECT) have been developed. However, an (18)F-labeled folic acid derivative suitable for positron emission tomography (PET) imaging that can be routinely applied is still lacking. In this study, a new fluorinated and radiofluorinated folic acid derivative, (18/19)F-click folate, was synthesized using click chemistry. In a convenient and very efficient two-step radiosynthesis, the isolated (18)F-click folate was obtained in good radiochemical yields of 25-35% with a specific activity of 160+/-70 GBq/micromol after
Language
  • English
Open access status
closed
Identifiers
Persistent URL
https://folia.unifr.ch/global/documents/154189
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