Biological activities of 4-fluoro estrogen analogues

J Steroid Biochem. 1983 Sep;19(3):1325-8. doi: 10.1016/0022-4731(83)90158-9.

Abstract

As part of a study on the biological activity of gamma-emitting estradiol analogues, a series of fluorinated and/or brominated analogues of estradiol were synthesized. 4-Fluoro-1,3,5(10-estratrien-3,17 beta-diol (4-fluoro-estradiol) and 16 alpha-bromo-1,3,5(10)-estratrien-3,17 beta-diol (16 alpha-bromo-estradiol) had relative binding affinities (RBA) for the rabbit uterine cytosol receptor which were comparable to those of estradiol. However, while 4-fluoro-estradiol stimulated the increase in uterine weight of immature mice to the same amount as estradiol, 16 alpha-bromo-estradiol was less effective in this assay indicating that its metabolism is probably more rapid than that of estradiol. 16 beta-Bromo-1,3,5(10)-estratrien-3,17 beta-diol had a low RBA and was ineffective in stimulating uterine weight at the doses used. 4-Fluoro-16 alpha-bromo-estradiol had a lower RBA than either the 4-fluoro- or 16 alpha-bromo-estradiol and all the 4-fluoro-seleno-estrogens tested possessed low RBA's.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Cytosol / metabolism
  • Estradiol / analogs & derivatives*
  • Estradiol / pharmacology
  • Female
  • Kinetics
  • Mice
  • Organ Size / drug effects
  • Rabbits
  • Receptors, Estrogen / metabolism*
  • Structure-Activity Relationship
  • Uterus / drug effects
  • Uterus / physiology*

Substances

  • Receptors, Estrogen
  • Estradiol