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Synthesis of potential estrogen-receptor based tumor-specific radiopharmaceuticals

Thesis/Dissertation ·
OSTI ID:5698067
Procedures were developed to label analogues of the nonsteroidal estrogen hexestrol with /sup 75/Se. Labeling was accomplished by substitution of divalent selenium for methylene. 1-Iodo-2,3-diphenylpentane and 1-iodo-2,3-bis(4-methoxyphenyl)pentane were synthesized and converted to their corresponding diselenides using NaH/sup 75/Se as nucleophile. The NaH/sup 75/Se was generated from (/sup 75/Se)selenious acid using NaBH/sub 4/ at pH 6.0. 1-(/sup 125/I)iodo-2,3-bis(4-methoxyphenyl)pentane was obtained from 2,3-bis(4-methoxyphenyl)pentane was obtained from 2,3-bis(4-methoxyphenyl)pentylmethanesulfonate using Na/sup 125/I in refluxing acetone. The cyclopropyl compound 1,1-dichloro-2,3-diphenylcyclotpropane was labeled with /sup 125/I at the 4-position on the aromatic ring. Labelling was accomplished by reacting 2,1-stilbeneazopyrrolidine synthesized from 4-nitrostilbene with Na/sup 125/I. Biodistribution studies in mature and immature female Sprague Dawley rats showed that the 1-methyl-(/sup 75/Se)seleno-2,3-bis(4-methoxyphenyl)pentane obtained slightly higher uterine-to-blood ratios and uterine tissue concentrations than did the other compounds.
Research Organization:
Oklahoma Univ., Oklahoma City (USA). Health Sciences Center
OSTI ID:
5698067
Country of Publication:
United States
Language:
English

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Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400702* -- Radiochemistry & Nuclear Chemistry-- Properties of Radioactive Materials
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BLOOD
BODY
BODY FLUIDS
CHEMICAL PREPARATION
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTROGENS
EVEN-ODD NUCLEI
FEMALE GENITALS
HORMONES
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MATERIALS
NUCLEI
ODD-EVEN NUCLEI
ORGANS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RODENTS
SELENIUM 75
SELENIUM ISOTOPES
STEROID HORMONES
SYNTHESIS
TISSUE DISTRIBUTION
UTERUS
VERTEBRATES