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  • Title: Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.
    Author: Miller JF, Gudmundsson KS, D'Aurora Richardson L, Jenkinson S, Spaltenstein A, Thomson M, Wheelan P.
    Journal: Bioorg Med Chem Lett; 2010 May 15; 20(10):3026-30. PubMed ID: 20443225.
    Abstract:
    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.
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