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EnglishFollowing 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.
| Titolo: | Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme |
| Autore/i: | GOBBI, SILVIA; CAVALLI, ANDREA; RAMPA, ANGELA; BELLUTI, FEDERICA; PIAZZI, LORNA; Paluszcak A.; Hartmann R. W.; RECANATINI, MAURIZIO; BISI, ALESSANDRA |
| Autore/i Unibo: | |
| Anno: | 2006 |
| Rivista: | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/jm060186y |
| 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. |
| Data prodotto definitivo in UGOV: | 2006-09-25 17:03:30 |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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