Figure 5

Hit compounds from the yeast-based Nef:Hck screen block HIV replication. A) U87MG/CD4/CXCR4 cells were infected with HIV strain NL4-3 in the presence of the top five compounds selected from the Nef:Hck-YEEI yeast screen shown in Figure 4C. Cells treated with the carrier solvent alone (DMSO) served as control. Release of viral p24 was determined in duplicate by ELISA four days post-infection, and the values shown reflect the mean percent of control ± S.D. B) Dose response curve for the anti-HIV activity of compound 2 from part A. Non-linear curve fitting was used to estimate an IC₅₀ value of 130 nM for this compound, which is a dihydrobenzo-1,4-dioxin-substituted analog of N-(3-aminoquinoxalin-2-yl)-4-chlorobenzenesulfonamide (DQBS; structure shown).