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Bioorg Med Chem Lett. 1998 May 5;8(9):1041-4.

Design and synthesis of a new type of non steroidal human aromatase inhibitors.

Author information

1
Centre d'Etudes et de Recherche sur le Médicament de Normandie, Laboratoire de Pharmacochimie, Caen, France.

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).

PMID:
9871704
DOI:
10.1016/s0960-894x(98)00157-7
[Indexed for MEDLINE]

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