Published in AIDS Weekly, May 24th, 2004
"A series of 6-aryl-2,4-dioxo-5-hexenoic acids were synthesized and tested against HIV-1 in cell-based assays and against recombinant HIV-1 integrase (rIN) in enzyme assays," wrote investigators in Italy.
"Compound 8a showed potent antiretroviral activity (EC50 = 1.5 mcM) and significant inhibition against ran (strand transfer: IC50 = 7.9 mcM; 3'-processing: IC50 = 7.0 mcM)," R. Costi and colleagues reported.
"A preliminary molecular modeling study was carried out to compare the spatial conformation of 8a with those of...
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