Anti-androgenic steroids

Details Anti-androgenic steroids Anti-androgenic steroids

1976-02-26

1977-11-22

Schwartz, Gerald A.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424311, 424331, 560256, C07C 4945

Patent

active

040596303

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.

REFERENCES:
federation Proceedings, vol. 34, No. 3, (Mar. 1, 1975), Batzold & Robinson.
Batzold & Robinson, J.A.C.S., vol. 97, p. 2576, (1975).
Batzold & Robinson, J. Org. Chem. 41, 313, (1976).
Carrell et al., American Crystallographic Assoc. Winter Meeting, Jan. 19, 1976, Clemson Univ., S. Carolina.

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