Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1909-11. doi: 10.1016/s0960-894x(00)00368-1.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 5-alpha Reductase Inhibitors*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Lactams / pharmacology*
  • Structure-Activity Relationship

Substances

  • 5-alpha Reductase Inhibitors
  • Enzyme Inhibitors
  • Lactams