[Steroid ligands of androgen binding protein. The enantiomers of trans-trans and cis-trans perhydrohexestrols and trans-trans perhydrodiketones]

J Steroid Biochem. 1982 Jul;17(1):101-12. doi: 10.1016/0022-4731(82)90599-4.
[Article in French]

Abstract

In the framework of a study on nonsteroidal androgens, the authors previously observed that in perhydrohexestrol series, the (+/-)-[(cis-4 hydroxycyclohexyl)-4(trans-4 hydroxycyclohexyl)-hexane] or cis-trans perhydrohexestrol and especially the (+/-)-(3,4 bis (trans-4-oxocyclohexyl)-hexane) or trans-trans perhydrodiketone, there is no affinity for AR (androgen receptor of the prostate) but they bind with high and specific affinity to the testosterone binding sites on ABP (epididymal androgen-binding protein). In this work, we describe the preparation, the stereochemistry and biological activities of trans-trans and cis-trans perhydrohexestrols and of trans-trans perhydrodiketone as well as their corresponding enantiomers. Biologically the tests AR and ABP are negative for the trans-trans perhydrohexestrol and of trans-trans perhydrodiketone and for its enantiomers. However for the enantiomers of cis-trans perhydrohexestrol and of trans-trans perhydrodiketone, the affinity of the (+) enantiomer for ABP is superior to that of the racemic and that of the (-) enantiomer, whereas the affinity for AR are zero. Chemically, the stereochemistry of the three racemics has been established by X-ray crystallographic analysis or by 1H n.m.r. The n.m.r. spectra have been analyzed in terms of chemical shifts and coupling constants.

Publication types

  • English Abstract
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androgen-Binding Protein / metabolism*
  • Animals
  • Binding Sites
  • Carrier Proteins / metabolism*
  • Crystallization
  • Epididymis / metabolism
  • Hexestrol / analogs & derivatives*
  • Hexestrol / metabolism
  • Magnetic Resonance Spectroscopy
  • Male
  • Prostate / metabolism
  • Rats
  • Rats, Inbred Strains
  • Stereoisomerism
  • X-Rays

Substances

  • Androgen-Binding Protein
  • Carrier Proteins
  • Hexestrol
  • perhydrodiketohexestrol
  • perhydrohexestrol