L. Kattner, S. Göhring, R. Hartmann
1995
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0
Influential Citations
8
Citations
Quality indicators
Journal
Archiv der Pharmazie
Abstract
Several (carbamoylalkenyl)‐ and (carbamoylalkenyl)phenyloxy carboxylic acids (Table 1) and some of their ethyl esters (Table 2) 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 %. Structure‐activity relationships are discussed.