Screening of potential cancer preventing chemicals as aromatase inhibitors in an in vitro assay.
The inhibition of human placental aromatase was used to rank a series of compounds, with the objective of selecting compounds for further evaluation as chemopreventive agents. (+/-)-p-Aminoglutethimide, introduced over two decades ago as a treatment for breast cancer, had an IC50 of 6.5 microM. Five compounds were more potent than aminoglutethimide in this assay: (+)- vorozole, 4-hydroxyandrostenedione, miconazole nitrate, plomestane, and 4-methoxy-androst-4-ene-3,17-dione. Other compounds with known chemoprevention activity, such as curcumin and genistein, were inactive. This assay for aromatase inhibitors is a rapid, economical way of ranking compounds for further development as chemoprevention agents.
White
E L
EL
Southern Research Institute, Birmingham, Alabama 35205, USA. white@sri.org
Ross
L J
LJ
Steele
V E
VE
Kelloff
G J
GJ
Hill
D L
DL
D016588:Anticarcinogenic Agents / Q000494:pharmacology*; D047072:Aromatase Inhibitors; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007654:Ketoconazole / Q000494:pharmacology
D016588:Anticarcinogenic Agents; D047072:Aromatase Inhibitors; D004791:Enzyme Inhibitors; D007654:Ketoconazole