期刊
MEDICINAL CHEMISTRY RESEARCH
卷 20, 期 2, 页码 200-209出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-010-9307-4
关键词
4-Hydroxy-pyran-2-ones; HIV-1 protease inhibitors; Anti-SIV activity
资金
- National Science Foundation of China [30670415]
In this study, we have modified 4-hydroxy-pyran-2-ones, especially introduced heteroatoms (S or O) into the substituents, and detected their interactions with the binding pockets of HIV-1 protease (PR). The results indicated that the ethoxyl groups at C-2' and C-5' of the phenyl ring could enhance the affinities to the S (1) ' and S (2) ' pockets and improve the inhibitory activities. The most potent compound 10f with an IC50 of 3.5 nM in enzymatic assay also exhibited good antiviral activity at the cellular level; it exhibited an EC50 value of 2.9 mu M in Simian immunodeficiency virus-infected CEM cells and suppressed the PR activity in 293T cells using western blot analysis.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据