Abortifacient, Antitumour/Estradienes: 11β-Arylsubstituted Steroids Showing Strong Binding to the Progesterone Receptor

Summary

Novelty: This is a continuation of AC0442 and discloses antigestational 11β-aryl-16α,17α-cyclohexano-estra-4,9-dienes. The compounds are competitive antagonists of the progesterone antigestation receptor and are suitable for inducing abortion and birth and for treating endometriosis, dysmenorrhoea and endocrine hormone dependent tumours (e.g. breast tumours).

Biology: The antigestation effect of the compounds has been determined in female pregnant rats. The compounds inhibited fertility up to 80% at a dose of 10mg/day. Their affinity for the progesterone receptor has also been evaluated. The relative binding affinity of the compounds was up to 470% compared to the standard (tritiated ORG 2058).

Chemistry: 16α, 17α-Cyclohexano-11β-(4-dimethylaminophenyl)-17β-hydroxymethylestra-4,9-diene-3-one is one of eight specifically claimed compounds.