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5. A New Class of Nonsteroidal Aromatase Inhibitors: Design and Synthesis of Chromone and Xanthone Derivatives and Inhibition of the P450 Enzymes Aromatase and 17α-Hydroxylase/C17,20-Lyase

Author

Recanatini, Maurizio, primary, Bisi, Alessandra, additional, Cavalli, Andrea, additional, Belluti, Federica, additional, Gobbi, Silvia, additional, Rampa, Angela, additional, Valenti, Piero, additional, Palzer, Martina, additional, Palusczak, Anja, additional, and Hartmann, Rolf W., additional

Published
2001
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10. Synthesis and biological evaluation of 3-(azolylmethyl)-1H-indoles and 3-(alpha-azolylbenzyl)-1H-indoles as selective aromatase inhibitors.

Author

Le Borgne M, Marchand P, Nourrisson MR, Loquet D, Palzer M, Le Baut G, and Hartmann RW

Subjects
Animals, Aromatase Inhibitors chemistry, Enzyme Activation drug effects, Female, Humans, Indoles chemistry, Inhibitory Concentration 50, Male, Microsomes chemistry, Microsomes drug effects, Molecular Structure, Placenta enzymology, Rats, Structure-Activity Relationship, Testis enzymology, Aromatase Inhibitors chemical synthesis, Aromatase Inhibitors pharmacology, Azoles chemistry, Indoles chemical synthesis, Indoles pharmacology, Steroid 17-alpha-Hydroxylase antagonists & inhibitors
Abstract

This present study identifies a number of azolyl-substituted indoles as potent inhibitors of aromatase. In the sub-series of 3-(azolylmethyl)-1H-indoles, four imidazole derivatives and their triazole analogues were tested. Imidazole derivatives 11 and 14 in which the benzyl moiety was substituted by 2-chloro and 4-cyano groups, respectively, were the most active, with IC50 values ranging between 0.054 and 0.050 microM. In the other sub-series, eight 3-(alpha-azolylbenzyl)-1H-indoles were prepared and tested. Compound 30, the N-ethyl imidazole derivative, proved to be an aromatase inhibitor, showing an IC50 value of 0.052 microM. All target compounds were further evaluated against 17alpha-hydroxylase/C17,20-lyase to determine their selectivity profile.

Published
2007
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