Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.
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.
Gobbi
Silvia
S
Cavalli
Andrea
A
Negri
Matthias
M
Schewe
Katarzyna E
KE
Belluti
Federica
F
Piazzi
Lorna
L
Hartmann
Rolf W
RW
Recanatini
Maurizio
M
Bisi
Alessandra
A
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
D047072:Aromatase Inhibitors; D001577:Benzophenones; D007093:Imidazoles; D013254:Steroid 17-alpha-Hydroxylase