Table 2.
The effect of the compounds against wild type HIV-1 replicationa.
| Compd | Ar | R1 | R2 | EC50±SD, μM | CC50±SD, μM | SI |
|---|---|---|---|---|---|---|
| CI - 39 | ![]() |
–OCH3 | – | 3.40 ± 0.45 | >30; (51.95 ± 4.29%) | >8.82 |
| CI-a | ![]() |
–H | – | >10; (91.98 ± 0.02%) | >30; (65.50 ± 5.49%) | – |
| CI-ba | – | – | – | >10; (82.96 ± 1.07%) | >30; (71.46 ± 4.41%) | – |
| CI-c | ![]() |
–OH | – | >10; (107.10 ± 7.63%) | 24.60 ± 3.79 | – |
| 5a | ![]() |
–OCH3 | – | >10; (113.22 ± 0.48%) | 27.98 ± 5.24 | – |
| 5b | ![]() |
–OCH3 | – | >10; (53.31 ± 3.18%) | >30; (62.74 ± 0.54%) | – |
| 5c | ![]() |
–OCH3 | – | >10; (124.35% ± 9.01%) | >30; (52.47 ± 5.34%) | – |
| 5d | ![]() |
–OCH3 | – | >10; (64.33 ± 0.23%) | >30; (68.50 ± 3.46%) | – |
| 5e | ![]() |
–OCH3 | – | >10; (109.33 ± 7.81%) | >30; (50.46 ± 1.22%) | – |
| 5f | ![]() |
–OCH3 | – | >10; (104.33 ± 3.96%) | >30; (72.64 ± 4.42%) | – |
| 5g | ![]() |
–OCH3 | – | >10; (60.76 ± 0.94%) | 29.08 ± 0.07 | – |
| 5h | ![]() |
–OCH3 | – | >10; (81.41 ± 3.79%) | >30; (54.00 ± 3.54%) | – |
| 5i | ![]() |
–OCH3 | – | >10; (72.89 ± 1.06%) | 28.58 ± 1.78 | – |
| 5j | ![]() |
–OCH3 | – | 3.30 ± 0.30 | 27.78 ± 3.57 | 8.42 |
| 5k | ![]() |
–OCH3 | – | >10; (113.00 ± 3.13%) | >30; (61.02 ± 5.24%) | – |
| 5l | ![]() |
–OCH3 | – | >10; (103.55 ± 3.27%) | >30; (51.01 ± 2.25%) | – |
| 5m | ![]() |
–OCH3 | – | 3.20 ± 0.40 | >30; (83.48 ± 5.27%) | >9.38 |
| 5n | ![]() |
–OCH3 | – | 4.40 ± 0.45 | >30; (67.04 ± 0.06%) | >6.82 |
| 5o | ![]() |
–OCH3 | – | >10; (71.46 ± 4.62%) | >30; (59.57 ± 0.05%) | – |
| 5p | ![]() |
–OCH3 | – | >10; (104.29 ± 0.82%) | >30; (86.68 ± 6.56%) | – |
| 5q | ![]() |
–OCH3 | – | >10; (128.61 ± 0.08%) | >30; (86.09 ± 7.19%) | – |
| 5r | ![]() |
–OCH3 | – | >10; (95.02 ± 2.76%) | >30; (51.62 ± 0.34%) | – |
| 5s | ![]() |
–OCH3 | – | >10; (87.28 ± 5.47%) | >30; (62.62 ± 4.79%) | – |
| 5t | ![]() |
–OCH3 | – | >10; (98.07 ± 0.36%) | 21.63 ± 0.07 | – |
| 5u | ![]() |
–OCH3 | – | >10; (47.94 ± 3.62%) | 13.86 ± 1.25 | – |
| 5vb | – | – | – | >10; (74.25 ± 7.59%) | 26.76 ± 1.50 | – |
| 5wc | – | – | – | >10; (82.07 ± 1.79%) | >30; (61.31 ± 3.32%) | – |
| 6a | ![]() |
–OCH2CH3 | – | 5.70 ± 0.10 | >30; (52.76 ± 2.56%) | >5.26 |
| 6b | ![]() |
–OCH2CH2CH3 | – | 6.70 ± 0.50 | >30; (55.39 ± 2.79%) | >4.48 |
| 6c | ![]() |
–OCH2CH3 | – | 0.86 ± 0.04 | 20.81 ± 2.13 | 24.20 |
| 6d | ![]() |
–OCH2CH2CH3 | – | 0.29 ± 0.01 | 29.49 ± 1.37 | 101.69 |
| 6e | ![]() |
–O(CH2)3CH3 | – | 0.64 ± 0.03 | 29.14 ± 0.74 | 45.53 |
| 6f | ![]() |
–O(CH2)4CH3 | – | 0.63 ± 0.03 | 18.73 ± 2.18 | 29.73 |
| 6g | ![]() |
–O(CH2)5CH3 | – | 1.02 ± 0.08 | >30; (56.95 ± 2.10%) | >29.41 |
| 6h | ![]() |
–O(CH2)6CH3 | – | 1.95 ± 0.05 | 23.88 ± 1.90 | 12.25 |
| 6i | ![]() |
–O(CH2)7CH3 | – | 4.40 ± 0.50 | 22.93 ± 3.21 | 5.21 |
| 6j | ![]() |
–O(CH2)8CH3 | – | >10; (58.30 ± 1.62%) | 28.85 ± 1.16 | – |
| 6k | ![]() |
–O(CH2)9CH3 | – | >10; (97.73 ± 1.22%) | >30; (52.80 ± 0.76%) | – |
| 6l | ![]() |
![]() |
– | 8.55 ± 0.95 | 16.50 ± 1.79 | 1.93 |
| 6m | ![]() |
![]() |
– | 5.50 ± 0.60 | >30; (49.31 ± 3.58%) | >5.45 |
| 6n | ![]() |
![]() |
– | >10; (73.20 ± 8.14%) | 20.28 ± 236 | – |
| 6o | ![]() |
![]() |
– | >10; (146.89 ± 10.59%) | 28.06 ± 0.11 | – |
| 6p | ![]() |
![]() |
– | >10; (113.06 ± 0.17%) | 29.43 ± 0.15 | – |
| 6q | ![]() |
–OCH2CH2CH3 | – | 4.28 ± 0.41 | 24.85 ± 3.06 | 5.81 |
| 10a | ![]() |
–OCH3 | – | >10; (138.11 ± 7.25%) | >30; (63.67 ± 4.32%) | – |
| 10b | ![]() |
–OCH3 | – | >10; (118.26 ± 7.86%) | >30; (78.70 ± 0.91%) | – |
| 10c | ![]() |
–OCH3 | – | 4.95 ± 0.35 | 14.27 ± 0.15 | 2.88 |
| 10d | ![]() |
–OCH3 | – | 0.53 ± 0.01 | 19.96 ± 0.86 | 37.66 |
| 10e | ![]() |
–OCH3 | – | 0.66 ± 0.06 | 18.55 ± 0.58 | 28.11 |
| 10f | ![]() |
–OCH2CH2CH3 | – | 0.06 ± 0.0005 | 16.41 ± 1.32 | 273.50 |
| 10g | ![]() |
–OCH2CH2CH3 | – | 0.33 ± 0.02 | 14.13 ± 0.13 | 42.82 |
| 10h | ![]() |
–OCH2CH2CH3 | – | 3.30 ± 0.00 | 17.92 ± 0.01 | 5.43 |
| 10i | ![]() |
–O(CH2)3CH3 | – | 0.06 ± 0.0005 | 22.06 ± 2.01 | 367.67 |
| 10j | ![]() |
–O(CH2)4CH3 | – | 0.13 ± 0.00 | 21.96 ± 1.99 | 168.92 |
| 14 | – | – | ![]() |
>10; (131.6 ± 0.60%) | 20.92 ± 5.11 | – |
| 15 | – | – | ![]() |
2.01 ± 0.06 | 18.98 ± 2.31 | 9.44 |
| 20a | – | – | ![]() |
>10; (99.48 ± 1.49%) | >30; (69.96 ± 0.41%) | – |
| 20b | – | – | ![]() |
>10; (65.67 ± 2.95%) | >30; (67.37 ± 6.75%) | – |
| 20c | – | – | ![]() |
>10; (93.41 ± 1.56%) | >30; (77.47 ± 3.25%) | – |
| NVP | – | – | – | 0.03 ± 0.003 | >30; (93.26 ± 0.68%) | >1000.00 |
| EFV | – | – | – | 0.0007 ± 0.0002 | 23.72 ± 4.45 | 33885.71 |

a: CI-b =
; b: 5v =
; c: 5w =
.
EC50: half maximal effective concentration; CC50: 50% cytotoxic concentration; SI: selectivity index.
The percentage in parentheses represents the infectivity or cell viability when treated with the compound at a final concentration of 10 μM or 30 μM.




























































