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Summary
Novelty: Novel 2,19-ethylene bridged steroid compounds which are steroidial aromatase inhibitors are disclosed. They are potentially useful for the treatment of hyperoestrogenaemia.
Biology: Enzyme kinetic analysis for the specified compound is said to have given a Ki = 23.9 nM.
Chemistry: The derivatives are prepared by cyclization of a 19[2-(4-toluene-sulphonyloxy) ethyl]androst-4-ene-3,17-dione using a strong base. The synthesis of nine compounds is described in detail and 2β,19-(ethylene)androst-4-ene-3,17-dione is one of four specifically claimed compounds.
Structure: