New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2, 3 or 5-(α-azolylbenzyl)-1H-indoles

M Le Borgne, P Marchand, B Delevoye-Seiller…

Index: Le Borgne, Marc; Marchand, Pascal; Delevoye-Seiller, Benedicte; Robert, Jean-Michel; Le Baut, Guillaume; Hartmann, Rolf W.; Palzer, Martina Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 3 p. 333 - 336

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Citation Number: 59

Abstract

Six azolyl substituted indoles were synthesized and tested for their activity to inhibit two P450 enzymes: P450 arom and P450 17α. It was observed that the introduction of α- imidazolylbenzyl chain at carbon 3 or 5 on indole nucleus led to very active molecules. Compounds 22, 23 and especially 33 demonstrate very high potential against P450 arom. Under our assay conditions of high substrate concentration the IC50 are 0.057, 0.0785 ...