Table 7.
Cytotoxicity and antiviral activity of tryptamine derivative 8 against HIV-1 and its NRTI- and NNRTI-resistant mutants.
| Compounds | CC50 a | EC50 b | |||||
|---|---|---|---|---|---|---|---|
| MT | HIV-1 | N119 | A17 | EFVR | AZTR | MDR | |
| 8 | 45 | 8.7 ± 0.8 | >45 | 12 ± 1.5 | >45 | 9.0 ± 1.0 | 9.0 ± 0.8 |
| Efavirenz | 40 | 0.002 ± 0.0003 | 0.018 ± 0.002 | 0.075 ± 0.009 | 7.0 ± 0.8 | 0.001 ± 0.0002 | NA |
| AZT | 45 | 0.022 ± 0.004 | 0.025 ± 0.004 | 0.01 ± 0.001 | 0.02 ± 0.001 | 0.35 ± 0.04 | 0.08 ± 0.006 |
| Nevirapine | >100 | 0.080 ± 0.005 | 6.3 ± 0.05 | 80 | 100 | 0.078 ± 0.008 | 5.0 ± 0.6 |
Data represent mean values for three independent determinations. a Compound concentration (µM) required to reduce the proliferation of mock-infected MT-4 cells by 50%. b Compound concentration (µM) required to achieve 50% protection of MT-4 cells from HIV-1 induced cytopathogenicity.