title: Synthesis and biological evaluation of 4-(4-(alkyl- and phenylaminocarbonyl)benzoyl)benzoic acid derivatives as non-steroidal inhibitors of steroid 5 alpha-reductase isozymes 1 and 2.
abstract: 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).
authors.affiliation: 8.5 Pharmaceutical and Medicinal Chemistry, Saarland University, P.O. Box 15 11 50, D-66041 Saarbrücken, Germany.
authors.forename: Ola I A
authors.initials: OI
authors.lastname: Salem
authors.forename: Tobias
authors.initials: T
authors.lastname: Schulz
authors.forename: Rolf W
authors.initials: RW
authors.lastname: Hartmann
mesh_terms: D058891:5-alpha Reductase Inhibitors; D000818:Animals; D001565:Benzoates / Q000138:chemical synthesis* / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D018120:Finasteride / Q000494:pharmacology; D006801:Humans; D007202:Indicators and Reagents; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D051381:Rats
chemical_list: D058891:5-alpha Reductase Inhibitors; D001565:Benzoates; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007527:Isoenzymes; D018120:Finasteride