Anti-androgenic steroids
AssigneeThe Johns Hopkins University
InventorCecil H. Robinson
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Abstract
The present invention relates to certain new and useful steroids which demonstrate anti-androgenic properties. These steroids are 5,10-secosteroids that have been found to be potent irreversible inhibitors of the enzyme .DELTA..sup.5 -3-ketosteroid isomerase which is involved in androgen biosynthesis. In addition, certain of the steroids of the invention compete reversibly with 5-.alpha.-dihydrotestosterone for binding to the prostatic cytoplasmic receptor protein while others inhibit the enzyme prostatic testosterone 5-.alpha.-reductase. The anti-androgenic properties of the present compounds indicate such utility as the control of abnormal growth of the human prostate, e.g. in the therapy of human prostatic cancer.
Claims3
A 5,10-secosteroid of the formula:
- ##STR14## wherein R.sup.1 is CH.sub.2 .dbd., O .dbd. or ##STR15## R.sup.2 is O .dbd., ##STR16## (where R.sup.3 is H or lower alkanoyl);
- ##STR17## (where R.sup.4 is H or lower alkanoyl);
- ##STR18## (where R.sup.5 is lower alkyl) or ##STR19## (where R.sup.6 is H, lower alkyl or Cl);
- and R.sup.7 is H or CH.sub.3.
5,10-secoestr-5-yne-3,10,17-trione.
5,10-seco-19-nor-pregn-5-yne-3,10,20-trione.
Dependencies are inferred from the claim text.