1. 2- and 3-[(aryl)(azolyl)methyl]indoles as potential non-steroidal aromatase inhibitors.
- Author
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Lézé MP, Le Borgne M, Marchand P, Loquet D, Kogler M, Le Baut G, Palusczak A, and Hartmann RW
- Subjects
- Androstenedione chemistry, Aromatase chemistry, Aromatase Inhibitors chemical synthesis, Aromatase Inhibitors chemistry, Drug Design, Drug Evaluation, Preclinical, Humans, Imidazoles chemistry, Imidazoles pharmacology, In Vitro Techniques, Indoles chemical synthesis, Indoles chemistry, Molecular Structure, Structure-Activity Relationship, Testosterone chemistry, Aromatase drug effects, Aromatase Inhibitors pharmacology, Indoles pharmacology
- Abstract
The present study was designed to follow our pharmacomodulation work in the field of non-steroidal aromatase inhibitors. All target compounds 12a-h and 28a-h were tested in vitro for human placental aromatase inhibition, using testosterone or androstenedione as the substrate for the aromatase enzyme and the IC50 and relative potency to aminoglutethimide data are included. A SAR study indicated that 3-[(4-fluorophenyl)(1H-imidazol-1-yl)methyl]-1-ethyl-2-methyl-1H-indole (28 g) was a highly potent and selective aromatase inhibitor with IC50 value of 0.025 microM. 28 g was also a weak inhibitor of androstenedione synthesis.
- Published
- 2004
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