2- and 3-[(aryl)(azolyl)methyl]indoles as potential non-steroidal aromatase inhibitors.

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.

Citation

Marie-Pierre Lézé, Marc Le Borgne, Pascal Marchand, Denis Loquet, Manuela Kogler, Guillaume Le Baut, Anja Palusczak, Rolf W Hartmann. 2- and 3-[(aryl)(azolyl)methyl]indoles as potential non-steroidal aromatase inhibitors. Journal of enzyme inhibition and medicinal chemistry. 2004 Dec;19(6):549-57

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PMID: 15662958

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