Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme
Journal of medicinal chemistry, 2006•ACS Publications
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.
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.
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.
ACS Publications以上显示的是最相近的搜索结果。 查看全部搜索结果