Table 2.
Anti-HIV activity and cytotoxicity of series II in MT-4 cells.
| ||||||||
|---|---|---|---|---|---|---|---|---|
| Compound ID | R1 | X | R4 | EC50 a (µM) | CC50 b (µM) | SI c | ||
| IIIB | ROD | IIIB | ROD | |||||
| 7g | H | CO | CH3 | 203.14 ± 10.98 | 184.07 ± 19.33 | >213.43 | >1.05 | >1.16 |
| 7h | H | SO2 | CH3 | 192.39 ± 3.17 | >201.06 | >201.06 | >1.05 | ND |
| 7i | H | CO | cyclopropyl | >167.50 | 15.02 ± 2.27 | 167.50 ± 19.81 | <1 | 11.15 |
| 7j | H | CO | CF3 | 157.50 ± 6.77 | 14.95 ± 4.83 | >195.42 | >1.24 | >13.08 |
| F2-7g | F | CO | CH3 | 177.40 ± 16.55 | 192.14 ± 4.57 | 196.03 ± 6.80 | 1.11 | 1.02 |
| F2-7h | F | SO2 | CH3 | 160.53 ± 15.43 | 183.40 ± 2.77 | >190.06 | >1.18 | >1.04 |
| F2-7i | F | CO | cyclopropyl | 14.36 ± 1.31 | 15.10 ± 0.68 | 88.56 ± 11.27 | 6.17 | 5.87 |
| F2-7j | F | CO | CF3 | 13.74 ± 0.70 | 16.55 ± 6.13 | 150.38 ± 25.46 | 10.95 | 9.09 |
| PF74 | 0.75 ± 0.33 | 4.16 ± 2.02 | 32.27 ± 2.94 | 43.03 | 7.76 | |||
a EC50: concentration of the test compound to attain 50% protection against HIV-induced cytotoxicity, determined by the MTT assay. b CC50: concentration of the test compound to reduce the viability of mock-infected cell cultures by 50%, determined by the MTT assay; values were averaged from at least three independent experiments. c SI: selectivity index, the ratio of CC50/EC50.