Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase.
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.
Abell
A D
AD
Department of Chemistry, University of Canterbury, Christchurch, New Zealand. a.abell@chem.canterbury.ac.nz
Prince
M J
MJ
McNulty
A M
AM
Neubauer
B L
BL
D058891:5-alpha Reductase Inhibitors; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007769:Lactams / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D058891:5-alpha Reductase Inhibitors; D004791:Enzyme Inhibitors; D007769:Lactams