Table 3.
Inhibitory Activities (IC50 Values) toward the 3′-End Processing and Strand Transfer Reactions Catalyzed by HIV-1 IN, DNA Binding Effects, anti-HIV Activities (EC50 Values, p24, and MTT assays) and Cytotoxicities (CC50 Values, MTT Assay) of the Peptides with Hydrophilic Sequences
| peptide | IC50 (μM) 3′-end processing |
IC50 (μM) strand transfer |
DNA binding effect (μM)a |
EC50 (μM) p24 assay |
EC50 (μM) MTT assay |
CC50(μM) MTT assay |
|---|---|---|---|---|---|---|
| 17 | 0.14 ± 0.02 | 0.056 ± 0.011 | 4 | 4.29 | 3.08 | 7.04 |
| 18 | 1.47 ± 0.18 | 0.81 ± 0.13 | 37 | 9.56 | 6.81 | >10 |
| 19 | 1.95 ± 0.25 | 1.13 ± 0.11 | 37 | >10 | >10 | >10 |
| 6S | 1.87 ± 0.14 | 0.71 ± 0.12 | 37 | 6.46 | 3.55 | >10 |
| 6L | N.T. | N.T. | N.T. | >10 | >10 | >10 |
| 8S | N.T. | N.T. | N.T. | (14.22) | 8.07 | >10 |
| 8L | N.T. | N.T. | N.T. | >10 | >10 | >10 |
| 5S | 2.6 ± 0.2 | 0.87 ± 0.14 | 37 | >10 | >10 | >10 |
| 1 | 1.62 ± 0.26 | 1.34 ± 0.2 | 37 | >10 | >10 | >10 |
| 2 | 0.119 ± 0.015 | 0.05 ± 0.004 | 4 | 3.51 | 4.54 | 5.91 |
| AZT | N.T. | N.T. | N.T. | 0.02 | 0.07 | >100 |
a
The lowest peptide concentrations that show retardation of DNA on wells of PAGE gels in integrase assays. That the same compounds give slightly different IC50 values, as shown in Tables 2-4 can be explained by the fact that batches of compounds were tested at different times and that overlapping compounds were used to ensure the reproducibility of the assays.