Gossypol and derivatives: a new class of aldose reductase inhibitors.
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.
Deck
L M
LM
Department of Biochemistry, University of New Mexico School of Medicine, Albuquerque 87131.
Vander Jagt
D L
DL
Royer
R E
RE
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006072:Gossypol / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D000449:Aldehyde Reductase; D006072:Gossypol