Table 2.
Anti-HIV (IIIB, RES056, and ROD) Activity and Cytotoxicity of 13a1–6, 13b1–5, 13c1–6, and 13d1–6
 |
|||||||
|---|---|---|---|---|---|---|---|
| compd | Ar | EC50(nM)a |
EC50 (μM)a |
SIc |
|||
| IIIB | RES056 | ROD | CC50 (μM)b | IIIB | RES056 | ||
| 13a1 | 4-SO2NH2-Ph | 4.3 ± 0.7 | 28.8 ± 1.2 | 6.55 ± 0.82 | 19.9 ± 10.1 | 4584 | 692 |
| 13a2 | 4-CONH2-Ph | 4.8 | 43.6 ± 5.0 | >165 | 165 ± 36.9 | 34162 | 3804 |
| 13a3 | 4-SO2CH3-Ph | 5.9 ± 1.3 | 46.6 ± 7.8 | 13.5 ± 9.00 | 11.9 ± 5.57 | 2025 | 257 |
| 13a4 | pyridine-4-yl | 2.6 ± 1.0 | 46.0 ± 1.9 | 15.7 ± 12.2 | ≥106 | ≥40104 | ≥2305 |
| 13a5 | 4-NO2-Ph | 8.0 ± 1.7 | 495 ± 1.3 | >6.18 | 6.18 ± 1.74 | 770 | 12 |
| 13a6 | 3-CONH2-Ph | 27.7 ± 21.5 | 629 ± 64.5 | >223 | ≥223 | ≥8048 | ≥355 |
| 13b1 | 4-SO2NH2-Ph | 37.2 ± 26.6 | 734 ± 337.2 | ≥26.7 | 26.6 ± 1.96 | 715 | 36 |
| 13b2 | 4-SO2Me-Ph | 3.8 ± 1.3 | 170 ± 32 | ≥22.7 | 45.3 ± 31.1 | 11690 | 259 |
| 13b3 | 4-NO2-Ph | 11.5 ± 0.4 | 1143 ± 108 | >27.1 | 27.1 ± 2.55 | 2341 | 24 |
| 13b4 | 4-NH2-Ph | 8.4 ± 2.8 | 704 ± 273 | 108 ± 53.3 | >256.9 | >30377 | >364 |
| 13b5 | 4-NHSO2Me-Ph | 11.2 ± 0.6 | 5240 ± 1500 | >257 | >256.9 | >19670 | >42 |
| 13c1 | 4-SO2NH2-Ph | 2.8 ± 1.0 | 38.0 ± 7.5 | ≥8.37 | 27.5 ± 7.49 | 9518 | 725 |
| 13c2 | 4-CONH2-Ph | 1.6 ± 0.4 | 41.5 ± 9.9 | 12.7 ± 0.72 | >250 | >156250 | >6039 |
| 13c3 | 4-SO2CH3-Ph | 1.9 ± 0.1 | 41.6 ± 4.9 | >27.0 | 31.3 ± 7.2 | 15946 | 752 |
| 13c4 | pyridine-4-yl | 2.3 ± 0.2 | 43.1 ± 1.2 | 5.12 ± 1.85 | 37.6 ± 11.0 | 15895 | 871 |
| 13c5 | 4-NO2-Ph | 7.4 ± 0.9 | 511 ± 165 | >11.1 | ≥11.1 | ≥1497 | ≥22 |
| 13c6 | 3-CONH2-Ph | 7.8 ± 3.4 | 1033 ± 51.1 | 209 ± 29.7 | >250 | >31780 | >243 |
| 13d1 | 4-SO2NH2-Ph | 1.1 ± 0.5 | 25.8 ± 1.19 | 58.3 ± 4.28 | >234 | >208333 | >9091 |
| 13d2 | 4-CONH2-Ph | 6.1 ± 2.7 | 173 ± 110 | 139 ± 24.3 | >251 | >40984 | >1448 |
| 13d3 | 4-SO2CH3-Ph | 4.9 ± 0.8 | 187 ± 0.79 | 41.8 ± 5.76 | 7.45 ± 0.93 | 1495 | 40 |
| 13d4 | pyridine-4-yl | 1.8 ± 0.7 | 54.7 ± 6.22 | 138 ± 25.7 | >274 | >147059 | >5020 |
| 13d5 | 4-NO2-Ph | 14.5 ± 3.6 | 941 ± 368 | >8.73 | 8.73 ± 3.53 | 599 | 9 |
| 13d6 | 3-CONH2-Ph | 2.0 ± 0.5 | 26786 | >205 | 205 ± 1.13 | 124410 | 9 |
| ETV | 5.1 ± 0.8 | 45.4 ± 15.5 | >4.59 | >889 | >101 | ||
a
EC50: concentration of compound required to achieve 50% protection of MT-4 cell cultures against HIV-1-induced cytopathic, as determined by the MTT method.
b
CC50: concentration required to reduce the viability of mock-infected cell cultures by 50%, as determined by the MTT method.
c
SI: selectivity index, the ratio of CC50/EC50.