303752-26-3Relevant articles and documents
Simple Bi- and tricyclic inhibitors of human steroid 5α-Reductase
Abell, Andrew D.,Prince, Maureen J.,McNulty, Ann M.,Neubauer, Blake L.
, p. 1909 - 1911 (2007/10/03)
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 5α-reductase. The tricycles with an 8-chloro substituent in the C-ring are nM (IC50) inhibitors of type 1 steroid 5α-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. (C) 2000 Elsevier Science Ltd.