Gossypol and derivatives: a new class of aldose reductase inhibitors

J Med Chem. 1991 Nov;34(11):3301-5. doi: 10.1021/jm00115a021.


Gossypol and 17 derivatives were tested as inhibitors of aldose reductase from human placenta. Gossypol and a number of the derivatives were potent inhibitors. The order of inhibitory activity was interpreted in relation to the Kador-Sharpless pharmacophor model for the aldose reductase inhibitor site. The structural but not the electronic aspects of the model were found to apply to this series of compounds.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Aldehyde Reductase / antagonists & inhibitors*
  • Aldehyde Reductase / isolation & purification
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Female
  • Gossypol / analogs & derivatives*
  • Gossypol / pharmacology
  • Humans
  • Structure-Activity Relationship


  • Enzyme Inhibitors
  • Aldehyde Reductase
  • Gossypol