Author/Authors :
P. Sonnet، نويسنده , , J. Guillon، نويسنده , , C. Enguehard، نويسنده , , P. Dallemagne، نويسنده , , R. Bureau، نويسنده , , S. Rault، نويسنده , , P. Auvray، نويسنده , , S. Moslemi، نويسنده , , P. Sourdaine، نويسنده , , S. Galopin and، نويسنده , , G. -E. Séralini، نويسنده ,
Abstract :
The structure-activity relationship study of one of recently described aromatase inhibitors, compound 1 (MR20814), allowed us to design some related derivatives as potential new inhibitors. Among those we synthesized, chlorophenylpyridylmethylenetetrahydroindolizinone 5 (MR20492) exhibited in vitro a ten-fold higher inhibition of the enzyme (IC50 = 0.2±0.0 μM and Ki = 10.3±3.3 nM).
