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3-Carboxy-20-keto steroids are dual uncompetitive inhibitors of human steroid 5α-reductase types 1 and 2

✍ Scribed by Dennis S. Yamashita; Dennis A. Holt; Hye-Ja Oh; Dinu Shah; Hwa-Kwo Yen; Martin Brandt; Mark A. Levy

Publisher
Elsevier Science
Year
1996
Tongue
English
Weight
321 KB
Volume
4
Category
Article
ISSN
0968-0896

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✦ Synopsis

Steroidal 3-carboxy-20-ketones have been prepared within two structural series, the androsta-3,5-dienes and the estra-1,3,5-trienes, as potential inhibitors of types 1 and 2 steroid 5 alpha-reductase, the enzyme activity responsible for the final step in biosynthesis of dihydrotestosterone. These compounds are shown to be potent uncompetitive inhibitors of both human recombinant enzyme activities, defining a novel class of dual steroid 5 alpha-reductase inhibitors.

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