Design and synthesis of a new type of non steroidal human aromatase inhibitors |
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| Authors: | P Sonnet J Guillon C Enguehard P Dallemagne R Bureau P Rault S Auvray S Moslemi P Sourdiane S Galopin GE Séralini |
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| Affiliation: | Centre d'Etudes et de Recherche sur le Médicament de Normandie, Laboratoire de Pharmacochimie, Caen, France. |
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| 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). |
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