Following our SAR studies on aromatase inhibitors, new compounds were designed by appropriately modifying the structure of flavone 1 using our previously reported CoMFA model. While the introduction of substituents on the 2-phenyl ring alone did not cause improvement in potency, these modifications and the removal of the 7-methoxy group led to compounds showing inhibitory activity in the nanomolar range, comparable to the marketed drug fadrozole.
Gobbi S., Cavalli A., Rampa A., Belluti F., Piazzi L., Paluszcak A., et al. (2006). Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme. JOURNAL OF MEDICINAL CHEMISTRY, 49, 4777-4780 [10.1021/jm060186y].
Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme
GOBBI, SILVIA;CAVALLI, ANDREA;RAMPA, ANGELA;BELLUTI, FEDERICA;PIAZZI, LORNA;RECANATINI, MAURIZIO;BISI, ALESSANDRA
2006
Abstract
Following our SAR studies on aromatase inhibitors, new compounds were designed by appropriately modifying the structure of flavone 1 using our previously reported CoMFA model. While the introduction of substituents on the 2-phenyl ring alone did not cause improvement in potency, these modifications and the removal of the 7-methoxy group led to compounds showing inhibitory activity in the nanomolar range, comparable to the marketed drug fadrozole.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
