Preparation and pharmacological profile of 7-(α-Azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors

P Marchand, M Le Borgne, M Palzer, G Le Baut…

Index: Marchand, Pascal; Le Borgne, Marc; Palzer, Martina; Le Baut, Guillaume; Hartmann, Rolf W. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 9 p. 1553 - 1555

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Citation Number: 32

Abstract

Aromatase (P450 arom) is a target of pharmacological interest for the treatment of breast cancer. New series of 7-(α-azolylbenzyl)-1H-indoles and indolines were synthesized as non- steroidal inhibitors of P450 arom. Selectivity was studied towards P450 17α enzyme. The most active compound, 1-ethyl-7-[(imidazol-1-yl)(4-chlorophenyl) methyl]-1H-indole 12c exhibited promising relative potency (rp) of 336 (rp of aminoglutethimide= 1) and most of ...