A novel class of inhibitors for steroid 5alpha-reductase: synthesis and evaluation of umbelliferone derivatives

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2361-3. doi: 10.1016/s0960-894x(01)00429-2.

Abstract

A series of umbelliferone derivatives was prepared and their 5alpha-reductase type 1 inhibitory activities were evaluated in cell culture systems. Our studies have identified a new series of potent 5alpha-reductase type 1 inhibitors and provided the basis for further development for the treatment of human endocrine disorders associated with overproduction of DHT by 5alpha-reductase type 1. The preliminary structure-activity relationship was described to elucidate the essential structural requirements.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 5-alpha Reductase Inhibitors*
  • Coumarins / chemistry*
  • Coumarins / pharmacology*
  • Drug Design
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Male
  • Prostatic Neoplasms / drug therapy
  • Structure-Activity Relationship
  • Tumor Cells, Cultured
  • Umbelliferones / chemistry*

Substances

  • 5-alpha Reductase Inhibitors
  • 8-allyl-7-hydroxy-2H-benzopyran-2-one
  • Coumarins
  • Enzyme Inhibitors
  • Umbelliferones
  • 7-hydroxycoumarin