Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.
@article{Singh2003ChemistryAS, title={Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.}, author={S. B. Singh and J. Ondeyka and W. Schleif and P. Felock and D. Hazuda}, journal={Journal of natural products}, year={2003}, volume={66 10}, pages={ 1338-44 } }
Integracides, 4,4-dimethylergostane triterpenoids, are inhibitors of HIV-1 integrase, a critical enzyme in replication of HIV-1. The chemistry and structure-activity relationship of integracide B and related natural products are described. A charged group, e.g., a sulfate, carboxyl, or amino, is required for the HIV-1 integrase activity. These compounds showed HIV-1 integrase activity with IC(50) values in the range 4.8-15 muM and exhibited antiviral activity in a viral spread assay, but with… CONTINUE READING
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