Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase |
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Authors: | Abell A D Prince M J McNulty A M Neubauer B L |
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Affiliation: | Department of Chemistry, University of Canterbury, Christchurch, New Zealand. a.abell@chem.canterbury.ac.nz |
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Abstract: | A number of tricyclic thiolactams, bicyclic lactams, and bicyclic thiolactams have been prepared and evaluated in vitro as inhibitors of types 1 and 2 steroid 5alpha-reductase. The tricycles with an 8-chloro substituent in the C-ring are nM (IC50) inhibitors of type 1 steroid 5alpha-reductase (SR). In all the cases studied, lactams are more potent than the corresponding thiolactams. Activity against type 2 SR is greatly enhanced by a styryl (or azo) substituent on the aryl ring of the tri- and bicycles and also a related tricyclic aryl acid. |
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