Synthesis and evaluation of a new series of 17alpha-[(123)I]iodovinyl estradiols.
A series of 17alpha-substituted estradiols was synthesized in which the stereochemical characteristics of carbons 20 and 21 were modified. It was found that the (Z)-isomer demonstrated more favorable receptor binding affinity than the corresponding (E)-isomer.
Kabalka
G W
GW
University of Tennessee Biomedical Imaging Center, Knoxville, Tennessee 37996-1600, USA. kabalka@utk.edu
Shoup
T M
TM
Daniel
G B
GB
Goodman
M M
MM
D000818:Animals; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D005260:Female; D007275:Injections, Intravenous; D007457:Iodine Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D011960:Receptors, Estrogen; D004958:Estradiol