Figure 5个  Table 3
    • Compound R1 R3 R4 R6 R7 HIV-1 infectivity (%) Cell survival rate (%)
      1 -CH2CH2N pyrrolidine OMe OMe OMe OMe 3.62±0.27 88.07±1.88
      2 -CH2CH2N piperidine OMe OMe OMe OMe 16.61±7.37 107.46±9.21
      3 -CH2CH2N-(CH2CH3)2 OMe OMe OMe OMe 47.78±4.35 86.89±1.97
      4 -CH2CH2N-(CH2CH3)2 OMe OMe H H 42.71±3.95 103.37±5.57
      5 -CH2CH2N piperidine OMe OMe OMe H 0.98±0.27 106.63±11.69
      6 -CH2CH2N piperidine OMe OMe H H 8.32±0.51 95.84±2.26
      7 -CH2CH2N piperidine NH2 H H H 18.69±0.00 74.18±1.17
      8 -CH2CH2N piperidine OMe OMe H F 0.48±024 85.50±7.76
      9 -CH2CH2N piperidine OMe OMe H Cl 1.65±0.25 93.67±2.12
      Seliciclib 45.01±1.99 103.57±4.30
      ID 262860 29.35±1.33 46.34±0.93
      The inhibitory effects on HIV-1 infection and cell viability were determined in TZM-bl cells infected with HIV-1NL4-3 at an MOI of 1.

      Table 1.  Structure and inhibitory effect of aristolactam derivatives 1–9 on HIV-1 infection.

    • Compound IC50 (μmol/L)a CC50 (μmol/L)b SIc
      1 0.69 ± 0.09 6.88 ± 0.31 9.94
      2 1.03 ± 0.38 16.91 ± 3.22 16.45
      3 3.73 ± 1.00 17.15 ± 0.34 4.59
      4 3.07 ± 0.22 6.98 ± 0.09 2.27
      5 1.07 ± 0.06 4.51 ± 0.96 4.23
      6 1.06 ± 0.03 4.97 ± 0.62 4.70
      7 2.00 ± 0.61 3.62 ± 0.15 1.80
      8 0.55 ± 0.01 3.72 ± 0.01 6.74
      9 0.44 ± 0.01 3.64 ± 0.08 8.31
      Seliciclib 2.29 ± 0.40 25.49 ± 0.17 11.11
      The inhibitory effects on HIV-1 infection and cell viability were determined in TZM-bl cells infected with HIV-1NL4-3 at an MOI of 1.
      aIC50: half-maximal inhibitory concentration.
      b CC50: concentration that reduces cell viability by 50%.
      cSI: selectivity index, i.e. the ratio of IC50 to CC50.

      Table 2.  Concentration–responses of aristolactam derivatives on cytotoxicity and anti-HIV activity.

    • Compound IC50 (μmol/L)a
      1 1.11 ± 0.02
      2 2.85 ± 0.17
      3 2.58 ± 0.05
      4 3.40 ± 0.02
      5 1.36 ± 0.01
      6 2.47 ± 0.26
      7 1.78 ± 0.15
      8 2.25 ± 0.24
      9 3.38 ± 0.05
      Seliciclib 2.25 ± 0.14
      aThe compounds were assessed in bl-DTR cells using a concentration–response test.

      Table 3.  Concentration–responses of aristolactam derivatives on the inhibition of Tat-induced HIV-1 transcription.