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. 2019 Sep 14;10(5):878–894. doi: 10.1016/j.apsb.2019.08.013

Table 2.

Activity against mutant HIV-1 strains of target compounds 11–32.

Compd. EC50 (nmol/L)a
L100I K103N Y181C Y188L E138K F227L + V106A RES056
11 89.3 ± 23.0 20.7 ± 2.75 63.5 ± 8.75 53.4 ± 2.15 49.9 ± 0.35 85.7 ± 9.71 565 ± 22.5
12 414 ± 37.9 129 ± 5.87 511 ± 77.2 307 ± 58.2 287 ± 4.98 1108 ± 269 2903 ± 119
13 186 ± 29.4 62.9 ± 10.4 197 ± 16.1 133 ± 3.35 193 ± 14.8 358 ± 18.4 1194 ± 184
14 262 ± 75.0 74.8 ± 2.93 180 ± 33.4 222 ± 30.5 177 ± 2.93 525 ± 21.1 813 ± 177
15 97.9 ± 62.4 23.1 ± 2.56 91.7 ± 18.2 106 ± 43.6 124 ± 88.7 56.7 ± 16.2 999 ± 151
16 731 ± 274 184 ± 90.2 731 ± 198 619 ± 3.59 662 ± 58.4 1092 ± 226 10,011 ± 1066
17 76.0 ± 17.2 17.9 ± 1.51 63.2 ± 16.1 62.0 ± 5.83 52.5 ± 11.3 56.8 ± 3.85 932 ± 88.4
18 925 ± 286 171 ± 56.9 741 ± 154 628 ± 49.6 739 ± 318 854 ± 186 4515 ± 1447
19 344 ± 117 59.9 ± 6.01 167 ± 24.5 121 ± 9.19 107 ± 18.8 200 ± 10.4 1713 ± 473
20 416 ± 87.9 102 ± 2.50 196 ± 54.6 205 ± 13.6 146 ± 12.5 395 ± 5.14 1733 ± 5.51
21 169 ± 2.91 57.6 ± 0.67 157 ± 5.61 146 ± 44.7 114 ± 9.20 122 ± 59.9 1563 ± 1280
22 268 ± 103 58.4 ± 7.14 158 ± 27.3 110 ± 3.57 149 ± 42.0 297 ± 39.8 1123 ± 353
23 45.4 ± 5.26 11.7 ± 1.03 44.8 ± 5.26 51.8 ± 8.47 30.9 ± 5.26 46.6 ± 15.5 388 ± 76.2
24 61.1 ± 9.35 11.7 ± 1.09 36.1 ± 1.21 51.4 ± 9.60 34.8 ± 10.6 56.6 ± 13.7 575 ± 120
25 27.4 ± 4.41 13.2 ± 0.33 30.8 ± 0.11 53.6 ± 3.50 44.4 ± 3.62 59.9 ± 10.2 103 ± 3.39
26 10.5 ± 4.56 6.02 ± 0.84 18.9 ± 2.28 23.9 ± 2.40 23.2 ± 8.64 97.2 ± 25.3 125 ± 39.3
27 24.6 ± 4.97 8.56 ± 1.69 32.4 ± 4.07 54.7 ± 2.26 34.8 ± 9.28 49.2 ± 8.26 347 ± 75.9
28 50.2 ± 10.3 20.0 ± 1.20 51.6 ± 4.32 73.4 ± 5.16 41.9 ± 4.56 157 ± 6.60 402 ± 41.9
29 247 ± 4.50 97.2 ± 3.07 260 ± 30.2 269 ± 30.0 183 ± 19.4 140 ± 1.31 1682 ± 388
30 1115 ± 543 173 ± 46.3 585 ± 33.3 556 ± 57.4 245 ± 173 1253 ± 804 >23,535
31 2401 ± 256 685 ± 0.21 2300 ± 413 1992 ± 46.5 979 ± 185 2157 ± 298 29,610 ± 4817
32 1135 ± 99.2 212 ± 7.34 626 ± 39.2 552 ± 45.6 198 ± 34.2 783 ± 196 4298 ± 1542
NVP 1403 ± 828 7818 ± 556 >9510 >9510 115 ± 24.5 >9510 >9510
EFV 46.5 ± 9.11 111 ± 35.4 6.33 ± 1.06 306 ± 53.9 5.12 ± 1.28 268 ± 48.7 265 ± 47.9
ETR 6.35 ± 1.77 3.13 ± 0.42 12.2 ± 2.63 17.3 ± 5.53 8.07 ± 2.52 14.2 ± 5.14 42.5 ± 15.1
K-5a2b 3.4 ± 0.6 2.9 3.2 ± 0.4 3.0 ± 0.1 2.9 4.2 ± 1.2 30.6 ± 12
a

EC50: concentration of compound required to achieve 50% protection of MT-4 cell cultures against HIV-1-induced cytotoxicity, as determined by the MTT method.

b

Data were reported in Ref. 14.