1. 2- and 3-[(Aryl)(azolyl)methyl]indoles as Potential Non-steroidal Aromatase Inhibitors.
- Author
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Lézé, Marie-Pierre, Le Borgne, Marc, Marchand, Pascal, Loquet, Denis, Kogler, Manuela, Le Baut, Guillaume, Palusczak, Anja, and Hartmann, Rolf W.
- Subjects
AROMATASE ,OXIDOREDUCTASES ,BREAST cancer ,TESTOSTERONE ,ENZYMES - Abstract
The present study was designed to follow our pharma-comodulation work in the field of non-steroidal aromatase inhibitors. All target compounds 12a-h and 28a-h were tested in vitro for human placental aroma-tase inhibition, using testosterone or androstenedione the substrate for the aromatase enzyme and the IC30 and relative potency to aminoglutethimide data are included. A SAR study indicated that 3-[(4-fluorophenyl)(1 Himidazol-1-yl) methyl]-1-ethyl-2-methyl-1H-indole (28g) was a highly potent and selective aromatase inhibitor with IC
50 value of 0.025 µM. 28 g was also a weak inhibitor of androstenedione synthesis. [ABSTRACT FROM AUTHOR]- Published
- 2004
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