کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1362996 | 981500 | 2010 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist](/preview/png/1362996.png)
Small molecules behaving as CD4 mimics were previously reported as HIV-1 entry inhibitors that block the gp120–CD4 interaction and induce a conformational change in gp120, exposing its co-receptor-binding site. A structure–activity relationship (SAR) study of a series of CD4 mimic analogs was conducted to investigate the contribution from the piperidine moiety of CD4 mimic 1 to anti-HIV activity, cytotoxicity, and CD4 mimicry effects on conformational changes of gp120. In addition, several hybrid molecules based on conjugation of a CD4 mimic analog with a selective CXCR4 antagonist were also synthesized and their utility evaluated.
SAR studies of CD4 mimics and their conjugation with a CXCR4 antagonist are reported.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 19, 1 October 2010, Pages 5853–5858