Anti-HIV activity of some synthetic lignanolides and intermediates
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- 作者：Sancho ; Rocí ; o ; Medarde ; Manuel ; Sá ; nchez-Palomino ; Sonsoles ; Madrigal ; Blanca M. ; et. al.
- 关键词：Anti-HIV-1 ; Synthetic lignanolides ; HIV-1 promoter activation ; HIV-1 Tat protein ; Transcription factor NF-κ ; B
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2004
- 出版时间：September 6, 2004
- 年：2004
- 卷：14
- 期：17
- 页码：4483-4486
- 全文大小：264 K
文摘
The evaluation of the anti-HIV-1 activity of synthetic lignanolides and their intermediates is reported. The antiviral activity was studied through luciferase-based assays targeting the HIV-1 promoter activation induced by either, the HIV-1 Tat protein or the cellular transcription factor NF-κB, both known as crucial factors in HIV-1 replication. Among the compounds tested, three of them 2, 4 and 13 were further analysed for their anti-HIV-1 activity by recombinant virus assays, showing a suitable profile for development of novel anti-HIV-1 drugs.