2- and 3-[(Aryl)(azolyl)methyl]indoles as Potential Non-steroidal Aromatase Inhibitors |
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Authors: | Marie-Pierre Lézé Pascal Marchand Denis Loquet Manuela Kogler Guillaume Le Baut |
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Affiliation: | Laboratoires de Chimie Organique et de Chimie Thérapeutique, UPRES EA 1155, Faculté de Pharmacie 1 rue Gaston Veil, F-44035, Nantes, France |
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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?μM. 28?g was also a weak inhibitor of androstenedione synthesis. |
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Keywords: | Aromatase 17-α-Hydroxylase/17,20-lyase Azoles Breast cancer |
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