TABLE 1.

Anti-HIV-1 activity of SDP derivatives

CompoundMean IC50 (IC90) ± SD in p24 assay (nM)CC50a (μM)
HIV-1Ba-L (R5)HIV-1JR-FL (R5)HIV-1MOKWb (R5)HIV-1MMb (R5MDR)HIV-1JSLb (R5MDR)HIV-1NL4-3 (X4)
AK6020.4 ± 0.3 (12 ± 10)0.1 ± 0.1 (4 ± 2)0.2 ± 0.1 (5 ± 3)0.6 ± 0.2 (11 ± 2)0.4 ± 0.3 (7 ± 2)>1,00050
AK53032 ± 27 (324 ± 120)13 ± 4 (144 ± 60)NDcNDND>1,00060
E91382 ± 58 (709 ± 256)81 ± 46 (>1,000)51 ± 14 (941 ± 201)61 ± 28 (>1,000)64 ± 30 (713 ± 405)>1,00050
E921/TAK-77928 ± 32 (256 ± 169)5 ± 1 (237 ± 25)11 ± 7 (194 ± 168)14 ± 8 (352 ± 180)7 ± 4 (316 ± 151)>1,00050
AK671/SCH-C4 ± 2 (79 ± 52)2 ± 0.5 (56 ± 57)2 ± 1 (54 ± 20)3 ± 0.5 (138 ± 25)2 ± 0.3 (84 ± 18)>1,000>100
Zidovudine7 ± 4 (48 ± 21)10 ± 9 (157 ± 72)6 ± 5 (47 ± 20)250 ± 98 (>1,000)70 ± 64 (>1,000)11 ± 5 (181 ± 90)>100
Nelfinavir12 ± 8 (105 ± 48)ND14 ± 8 (82 ± 56)>1,000>1,00020 ± 7 (75 ± 52)ND
Saquinavir11 ± 5 (60 ± 21)ND5 ± 2 (49 ± 40)300 ± 65 (>1,000)350 ± 105 (>1,000)10 ± 4 (48 ± 2)ND
  • a Cytotoxic concentrations of a compound that reduces the number of cells by 50% (CC50) were determined as previously reported (17).

  • b HIV-1MOKW was isolated from a drug-naive AIDS patient (17), while HIV-1MM and HIV-1JSL were from patients who received antiretroviral therapy for a long period and whose virus acquired a number of mutations in the RT- and PR-encoding HIV-1 genes (36).

  • c ND, not determined.