Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371721 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Using AMD070 as a starting point for structural modification, a novel series of isoquinoline CXCR4 antagonists was developed. A structure–activity scan of alternate lower heterocycles led to the 3-isoquinolinyl moiety as an attractive replacement for benzimidazole. Side chain optimization in the isoquinoline series led to a number of compounds with low nanomolar anti-HIV activities and promising rat PK properties.
Graphical abstractUsing AMD070 as a starting point for structural modification, a novel series of isoquinoline CXCR4 antagonists was developed. A structure–activity scan of alternate lower heterocycles led to the 3-isoquinolinyl moiety as an attractive replacement for benzimidazole. Side chain optimization in the isoquinoline series led to a number of compounds with low nanomolar anti-HIV activities and promising rat PK properties.Figure optionsDownload full-size imageDownload as PowerPoint slide