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 S., Cavalli A., Negri M., Schewe K.E., Belluti F., Piazzi L., et al. (2007). Imidazolylmethylbenzophenones as highly potent aromatase inhibitors. JOURNAL OF MEDICINAL CHEMISTRY, 50, 3420-3422 [10.1021/jm0702938].
Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.
GOBBI, SILVIA;CAVALLI, ANDREA;BELLUTI, FEDERICA;PIAZZI, LORNA;RECANATINI, MAURIZIO;BISI, ALESSANDRA
2007
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
