Table 2

Inhibitory effects of control compounds DS, AZT, Ro5-3335, and Saquinavir and AdoHcy hydrolase inhibitors on HIV-1 replication

Inhibition of virus-induced LacZ expression, IC502-aToxicity, CC502-b
μm
DS 50000.007  ± 0.001>2
AZT0.00034  ± 0.000022>0.04
Ro5-33350.1  ± 0.053.36  ± 2.58
Saquinavir0.8  ± 0.5>15
NPA1.9  ± 2.730  ± 31
c3NPA0.41  ± 1.576  ± 21
DHCaA1.3  ± 1 55
c3DHCaA0.29  ± 0.004237  ± 25
C-c3Ado7.4  ± 5>37
6′-(R)-Methyl-NPA3.5  ± 0.5>36
6′-(S)-Methyl-NPA>36 >36
(S)-DHPA248  ± 189>191
c7DHCaA 51 >42
6′-(R)-Ethynyl-NPA 38 >69
6′-(S)-Ethynyl-NPA>104>104
6′-(R)-Ethenyl-NPA6.16  ± 3>69
6′-(S)-Ethenyl-NPA57  ± 52>138
6′-(R)-Ethyl-NPA4.6  ± 0.34>68
6′-(S)-Ethyl-NPA67  ± 3.7>68
  • 2-a Concentration of the inhibitor required for 50% inhibition of β-Gal expression driven by the HIV-1 LTR in HIV-1-infected CD4+ HeLa cells.

  • 2-b Concentration of the inhibitor required for 50% inhibition of total protein expression in cell culture.

  • Data represent mean values of two to four separate experiments, each performed in triplicate.