title: Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.
abstract: Suppression of tumor and plasma estrogen levels by inhibition of aromatase is one of the most effective treatments for postmenopausal breast cancer patients. Starting from an easy, synthetically accessible, benzophenone scaffold, a new class of potent aromatase inhibitors was synthesized, endowed with high selectivity with respect to 17 alpha-hydroxylase/17,20-lyase (CYP17). Compounds 1b and 1d proved to be among the most potent inhibitors described so far.
authors.forename: Silvia
authors.initials: S
authors.lastname: Gobbi
authors.forename: Andrea
authors.initials: A
authors.lastname: Cavalli
authors.forename: Matthias
authors.initials: M
authors.lastname: Negri
authors.forename: Katarzyna E
authors.initials: KE
authors.lastname: Schewe
authors.forename: Federica
authors.initials: F
authors.lastname: Belluti
authors.forename: Lorna
authors.initials: L
authors.lastname: Piazzi
authors.forename: Rolf W
authors.initials: RW
authors.lastname: Hartmann
authors.forename: Maurizio
authors.initials: M
authors.lastname: Recanatini
authors.forename: Alessandra
authors.initials: A
authors.lastname: Bisi
mesh_terms: D047072:Aromatase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001577:Benzophenones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001665:Binding Sites; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D008958:Models, Molecular; D010920:Placenta / Q000648:ultrastructure; D011485:Protein Binding; D013254:Steroid 17-alpha-Hydroxylase / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D047072:Aromatase Inhibitors; D001577:Benzophenones; D007093:Imidazoles; D013254:Steroid 17-alpha-Hydroxylase