TABLE 1.

Anti-HIV activity of betulinic acid derivatives

VirusaIC50 of indicated compound (μM)b
DSBIC9564LH55LH15
NL4-30.096 ± 0.0120.11 ± 0.020.0065 ± 0.00080.016 ± 0.003
PI-R1.71 ± 0.150.12 ± 0.030.032 ± 0.0040.049 ± 0.005
RTI-R0.085 ± 0.0080.093 ± 0.0160.01 ± 0.0010.019 ± 0.003
  • a PI-R is an HIV-1 strain, HIV-1M46I/L63P/V82P/I84V, resistant to multiple protease inhibitors (2). RTI-R is an HIV-1 strain, HIV-1RTMDR1/MT2 (RT 74V, 41L, 106A, 215Y), resistant to multiple HIV-1 reverse transcriptase inhibitors (10). PI-R and RTI-R were obtained from the National Institutes of Health AIDS Research and Reference Reagent Program.

  • b IC50 is the drug concentration required to inhibit 50% of HIV-1 replication. The highest concentration tested for these compounds was 5 μM; there was no observable cytotoxicity at this concentration. The numbers in the table represent the means ± the standard deviations of three independent experiments done in duplicate.