Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors |
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| Authors: | Lézé Marie-Pierre Palusczak Anja Hartmann Rolf W Le Borgne Marc |
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| Affiliation: | Université de Nantes, Nantes Atlantique Universités, Département de Pharmacochimie, IICiMed UPRES EA 1155, UFR de Sciences Pharmaceutiques, 1 rue Gaston Veil, Nantes, F-44035 Cedex 1, France. |
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| Abstract: | Two new series of benzonitrile derivatives on position 6 or 4 of indole ring were successfully synthesized via a Leimgruber-Batcho reaction. All the compounds were evaluated in vitro on the inhibition of aromatase (CYP19) and 17alpha-hydroxylase-C17,20-lyase (CYP17). The racemate, 4-[(1H-imidazol-1-yl)(1H-indol-4-yl)methyl]benzonitrile 9, showed high level of inhibitory activity towards CYP19 (IC(50)=11.5 nM). |
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