Title of article
Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: Potent and selective aromatase inhibitors
Author/Authors
Marie-Pierre Lézé، نويسنده , , Marc Le Borgne، نويسنده , , Patricia Pinson، نويسنده , , Anja Palusczak، نويسنده , , Muriel Duflos، نويسنده , , Guillaume Le Baut، نويسنده , , Rolf W. Hartmann، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
1134
To page
1137
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 (IC50 = 15.3 nM). Chiral chromatography allowed isolation of the (+) enantiomer 8b2, which was about twice as active as the racemate (IC50 = 9 nM).
Keywords
breast cancer , Aromatase inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796529
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