Archiv der Pharmazie p. 239 - 245 (1995)
Update date:2022-07-29
Topics:
Kattner
Gohring
Hartmann
Several (carbamoylalkenyl)- and (carbamoylalkenyl)phenyloxy carboxylic acids and some of their ethyl esters were synthesized and evaluated in vitro as inhibitors of steroid 5α-reductase. Inhibitors of this enzyme may be useful in treating dihydrotestosterone-related diseases such as prostate cancer and benign prostatic hyperplasia. Using an enzyme preparation obtained from human prostate carcinoma tissue, the inhibition values ranged from 0 to 57% at the given dose of 100 μM. In the series of free acids, surprisingly, the compounds showed only modest inhibitory potency (0-26%). By contrast, the ethyl esters displayed inhibition values up to 57%. Sttructure-activity relationships are discussed.
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