(Development of Br-77 from LAMPF Facility)

Technical Report · Tue Jan 01 00:00:00 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
62 RADIOLOGY AND NUCLEAR MEDICINE
59 BASIC BIOLOGICAL SCIENCES
ESTRADIOL
HALOGENATION
LABELLED COMPOUNDS
SYNTHESIS
NEOPLASMS
RADIOTHERAPY
STEROIDS
LABELLING
AFFINITY
BROMINE 77
CRYSTALLOGRAPHY
ESTROGENS
HALIDES
MAMMARY GLANDS
PROGRESS REPORT
RADIOPHARMACEUTICALS
RATS
RECEPTORS
THERAPEUTIC USES
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BROMINE ISOTOPES
CHEMICAL REACTIONS
DAYS LIVING RADIOISOTOPES
DISEASES
DOCUMENT TYPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRANES
GLANDS
HALOGEN COMPOUNDS
HORMONES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
ISOTOPES
MAMMALS
MEDICINE
MEMBRANE PROTEINS
MINUTES LIVING RADIOISOTOPES
NUCLEAR MEDICINE
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PROTEINS
RADIOISOTOPES
RADIOLOGY
RODENTS
STEROID HORMONES
THERAPY
USES
VERTEBRATES
400703* - Radiochemistry & Nuclear Chemistry- Radioisotope Production
550604 - Medicine- Unsealed Radionuclides in Therapy- (1980-)
550201 - Biochemistry- Tracer Techniques