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论文题目: Synthesis of Quinolin-2-one Alkaloid Derivatives and Their Inhibitory Activities against HIV-1 Reverse Transcriptase
作者: 程辟 曾建国*
刊物名称: Molecules
卷: 16
期: 6
页码: 7649-7661
发表时间: 2011-6-16
摘要:

 

 

 

Abstract: Based on an established common pharmacophore of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNTTIs), a series of quinolin-2-one derivatives were synthesized and assayed for their in vitro activities against HIV-1 reverse transcriptase (RT) for the first time. Some of the tested compounds were active against HIV-1 RT. Compounds 4a2 and 4d2 showed inhibitory activities with IC50 values of 0.21 and 0.15 mM, respectively, with a mode of interaction with RT residues of the allosteric pocket similar to that of efavirenz.
Keywords: quinolin-2-one; alkaloid; synthesis; HIV-1 RT; activity
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