Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: potent and selective aromatase inhibitors |
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| Authors: | Lézé Marie-Pierre Le Borgne Marc Pinson Patricia Palusczak Anja Duflos Muriel Le Baut Guillaume Hartmann Rolf W |
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| Institution: | Department of Pharmacochemistry, BioCiT UPRES EA1155, Faculty of Pharmacy, Nantes University, 1 rue Gaston Veil, F-44035 Nantes Cedex, France. mpl_leze@yahoo.fr |
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| Abstract: | The synthesis and the aromatase (CYP19) inhibitory activity of 5-(aryl)(imidazol-1-yl)methyl]-1H-indoles were reported. Among the tested racemate compounds, 5-(4-chlorophenyl)(1H-imidazol-1-yl)methyl]-1H-indole 8b emerged as a potent CYP19 inhibitor (IC(50)=15.3 nM). Chiral chromatography allowed isolation of the (+) enantiomer 8b2, which was about twice as active as the racemate (IC(50)=9 nM). |
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