title: Design and synthesis of a new type of non steroidal human aromatase inhibitors.
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).
authors.affiliation: Centre d'Etudes et de Recherche sur le Médicament de Normandie, Laboratoire de Pharmacochimie, Caen, France.
authors.forename: P
authors.initials: P
authors.lastname: Sonnet
authors.forename: J
authors.initials: J
authors.lastname: Guillon
authors.forename: C
authors.initials: C
authors.lastname: Enguehard
authors.forename: P
authors.initials: P
authors.lastname: Dallemagne
authors.forename: R
authors.initials: R
authors.lastname: Bureau
authors.forename: P
authors.initials: P
authors.lastname: Rault S Auvray
authors.forename: S
authors.initials: S
authors.lastname: Moslemi
authors.forename: P
authors.initials: P
authors.lastname: Sourdiane
authors.forename: S
authors.initials: S
authors.lastname: Galopin
authors.forename: G E
authors.initials: GE
authors.lastname: Séralini
mesh_terms: D047072:Aromatase Inhibitors; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D017316:Fadrozole / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D006801:Humans; D007202:Indicators and Reagents; D007212:Indolizines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008861:Microsomes / Q000201:enzymology; D010920:Placenta / Q000201:enzymology; D011247:Pregnancy; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology
chemical_list: D047072:Aromatase Inhibitors; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007212:Indolizines; C116636:MR 20492; D011725:Pyridines; D014230:Triazoles; C060523:vorozole; D017316:Fadrozole