排序方式: 共有1条查询结果,搜索用时 0 毫秒
1
1.
MARC LE BORGNE PASCAL MARCHAND MARIE-RENEE NOURRISSON DENIS LOQUET MARTINA PALZER GUILLAUME LE BAUT 《Journal of enzyme inhibition and medicinal chemistry》2013,28(5):667-676
This present study identifies a number of azolyl-substituted indoles as potent inhibitors of aromatase. In the sub-series of 3-(azolylmethyl)-1H-indoles, four imidazole derivatives and their triazole analogues were tested. Imidazole derivatives 11 and 14 in which the benzyl moiety was substituted by 2-chloro and 4-cyano groups, respectively, were the most active, with IC50 values ranging between 0.054 and 0.050 μM. In the other sub-series, eight 3-(α-azolylbenzyl)-1H-indoles were prepared and tested. Compound 30, the N-ethyl imidazole derivative, proved to be an aromatase inhibitor, showing an IC50 value of 0.052 μM. All target compounds were further evaluated against 17α-hydroxylase/C17,20-lyase to determine their selectivity profile. 相似文献
1