Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1362996 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
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.
Graphical abstractSAR studies of CD4 mimics and their conjugation with a CXCR4 antagonist are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide