Radiobrominated triphenylethylenes as estrogen receptor binding radiopharmaceuticals
Estrogen receptor binding radiopharmaceuticals have potential for use in the diagnosis and treatment of cancers of the female reproductive system. Tamoxifen is an antiestrogen derived from the triphenylethylene skeleton which is used in the treatment of mammary carcinoma. Hydroxytamoxifen is a metabolite of tamoxifen which binds tightly to the estrogen receptor. Two triphenylethylene derivatives based on the structure of hydroxytamoxifen have been prepared: 1-bromo-1-phenyl-2- (2-dimethylamino)-4-ethoxyphenyl -2-(4-hydroxyphenyl) ethene (1) where the ethyl group of hydroxytamoxifen has been replaced by a bromine, and 1-bromo-1-phenyl-2,2-(4-hydroxyphenyl) ethene (2) with a similar substitution and also lacking the aminoethoxy side chain believed to confer antiestrogenicity. Both 1 and 2 bind strongly to the estrogen receptor. 2 has been labeled with the Auger electron emitting nuclide Br-80m in moderate yields in high specific activity using either N-bromosuccinimide or N-bromophthalimide and shows promise as a potential radiotherapy agent.
- Research Organization:
- Michael Reese Hospital and Medical Center, The Univ. of Chicago Medical Center, Chicago, IL
- OSTI ID:
- 7030645
- Report Number(s):
- CONF-850611-; TRN: 87-010789
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 26:5; Conference: 32. annual meeting of the Society of Nuclear Medicine, Houston, TX, USA, 2 Jun 1985
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
BROMINE 80
RADIOCHEMISTRY
ESTROGENS
RECEPTORS
TAMOXIFEN
BROMINATION
CHEMICAL PREPARATION
STRUCTURE-ACTIVITY RELATIONSHIPS
AUGER EFFECT
BINDERS
BROMINE 88
CHEMICAL BONDS
CHEMICAL REACTION YIELD
DERIVATIZATION
DIAGNOSIS
ETHYLENE
FEMALE GENITALS
HYDROXY COMPOUNDS
IMIDES
LABELLING
NEOPLASMS
PHTHALIC ACID
RADIOACTIVATION
RADIOPHARMACEUTICALS
SUCCINIC ACID
ALKENES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BROMINE ISOTOPES
CARBOXYLIC ACIDS
CHEMICAL REACTIONS
CHEMISTRY
DICARBOXYLIC ACIDS
DISEASES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
HALOGENATION
HORMONES
HOURS LIVING RADIOISOTOPES
HYDROCARBONS
INTERMEDIATE MASS NUCLEI
INTERNAL CONVERSION RADIOISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MEMBRANE PROTEINS
MINUTES LIVING RADIOISOTOPES
NUCLEI
ODD-ODD NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
RADIOISOTOPES
SECONDS LIVING RADIOISOTOPES
STEROID HORMONES
SYNTHESIS
YIELDS
550601* - Medicine- Unsealed Radionuclides in Diagnostics
550604 - Medicine- Unsealed Radionuclides in Therapy- (1980-)
400700 - Radiochemistry & Nuclear Chemistry