| Literature DB >> 1901911 |
C Piantadosi1, C J Marasco, S L Morris-Natschke, K L Meyer, F Gumus, J R Surles, K S Ishaq, L S Kucera, N Iyer, C A Wallen.
Abstract
Combinations of an amidoalkylphosphocholine, 8, and AZT have been found to cause an apparent synergistic action in suppressing infectious HIV-1 replication. In addition, amidoalkyl, oxyalkyl, and thioalkyl ether lipids have been chemically linked to anti-HIV-1 nucleosides (AZT and DDI) through phosphate and phosphonate linkages. These conjugates have shown promising in vitro anti-HIV-1 activity. Also, the conjugates have a 5-10-fold reduction in cell cytotoxicity compared to AZT alone. The most active compound, an amidoalkyl ether lipid-AZT conjugates, 4A, was found to have a differential selectivity of 1793 in a syncytial plaque assay. In comparison, AZT alone has a value of 1281.Entities:
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Year: 1991 PMID： 1901911 DOI： 10.1021/jm00108a025
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446