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Synthesis and Biological Evaluation of 4-(4-(Alkyl-and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-steroidal Inhibitors of Steroid 5α-Reductase Isozymes 1 and 2

✍ Scribed by Ola I. A. Salem; Tobias Schulz; Rolf W. Hartmann

Publisher: John Wiley and Sons
Year: 2002
Tongue: English
Weight: 115 KB
Volume: 335
Category: Article
ISSN: 0365-6233
DOI: 10.1002/1521-4184(200203)335:2/3<83::aid-ardp83>3.0.co;2-3

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✦ Synopsis

The synthesis and biological evaluation of 4-(4-(alkyl- and phenylaminocarbonyl)benzoyl)benzoic acids (4a-4d) as non-steroidal inhibitors of steroid 5 alpha-reductase are described. The compounds were tested in vitro for inhibitory activity toward rat and human 5 alpha-reductase isozymes 1 and 2 at a concentration of 10 microM. The most active inhibitor for the human type 2 isozyme was 4-(4-(phenylaminocarbonyl)benzoyl)benzoic acid, compound 4c (IC50 = 0.82 microM).

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