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ID: ALA1130802
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of a new type of non steroidal human aromatase inhibitors.
Authors: Sonnet P, Guillon J, Enguehard C, Dallemagne P, Bureau R, Rault S Auvray P, Moslemi S, Sourdiane P, Galopin S, Séralini GE.
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 microM and Ki = 10.3 +/- 3.3 nM).
CiteXplore: 9871704