(Development of Br-77 from LAMPF Facility)

Technical Report · Tue Jan 01 04:00:00 EST 1985

DOI:https://doi.org/10.2172/6806687· OSTI ID:6806687

The research goals of 1984--1985 included continued studies of the 1-halogenated estradiol derivatives and preparation of B- and C- ring vinyl halides of estradiol. The radiohalogenated analogs of these target compounds are proposed to be useful as receptor-binding radiopharmaceuticals in breast cancer therapy. To date, all 1-halogenated derivatives have been prepared and studied. Their 17 {proportional to}-ethynyl derivatives have also been prepared. In vitro receptor-binding studies with estrogen receptors show definite trends with respect to type of halogen attached versus observed receptor-binding affinity. These results were further substantiated using x-ray crystallographic methods. The proposed B- and C- ring vinyl halides have not been successfully synthesized; however, work toward these target compounds is still underway. Other related compounds of current interest include the B-, C-, and D- ring substituted estradiol derivatives. Much of the synthetic work leaking to these compounds has been accomplished and in vitro studies will be performed soon. 10 refs.

• Research Organization: New Mexico Univ., Albuquerque, NM (USA). School of Medicine
• Sponsoring Organization: DOE/ER
• DOE Contract Number: AS04-81EV10596
• OSTI ID: 6806687
• Report Number(s): DOE/EV/10596-T5; ON: DE91000116
• Country of Publication: United States
• Language: English

Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
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59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AFFINITY
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BROMINE 77
BROMINE ISOTOPES
CHEMICAL REACTIONS
CRYSTALLOGRAPHY
DAYS LIVING RADIOISOTOPES
DISEASES
DOCUMENT TYPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRADIOL
ESTRANES
ESTROGENS
GLANDS
HALIDES
HALOGEN COMPOUNDS
HALOGENATION
HORMONES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
ISOTOPES
LABELLED COMPOUNDS
LABELLING
MAMMALS
MAMMARY GLANDS
MEDICINE
MEMBRANE PROTEINS
MINUTES LIVING RADIOISOTOPES
NEOPLASMS
NUCLEAR MEDICINE
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PROGRESS REPORT
PROTEINS
RADIOISOTOPES
RADIOLOGY
RADIOPHARMACEUTICALS
RADIOTHERAPY
RATS
RECEPTORS
RODENTS
STEROID HORMONES
STEROIDS
SYNTHESIS
THERAPEUTIC USES
THERAPY
USES
VERTEBRATES