Table 2.
Cytotoxicity (EC50) of studied compounds to selected cell lines
Compound | EC50 [μM] | ||||
---|---|---|---|---|---|
No. | Designation | Rat glioma (C6) |
Mouse fibroblasts (A9) |
Human dermal fibroblasts (HDF) | Human embryonic kidney (Hek293) |
1 | H-Box[(4-Me)Ph]-OMe | 309 ± 7 | nd | nd | nd |
2 | H-Box[(4-F)Ph]-OMe | 372 ± 3 | nd | nd | nd |
3 | H-Box[(4-CN)Ph]-OMe | 286 ± 7 | nd | nd | nd |
4 | H-Box[(4-COOH)Ph]-OMe | No effect | nd | nd | nd |
5 | H-Box[(4-Br)Ph]-OMe | 230 ± 1 | 80 ± 5 | 46 ± 0.3 | 238 ± 15 |
6 | H-Box[(2-OMe)Ph]-OMe | 438 ± 20 | 334 ± 22 | 100 ± 2 | 718 ± 92 |
7 | H-Box[2,5-(OMe)2Ph]-OMe | 900 ± 21 | 354 ± 33 | 60 ± 4 | 256 ± 21 |
8 | H-Box[2,4,5-(OMe)3Ph]-OMe | 832 ± 58 | 1700 ± 25 | 238 ± 9 | 745 ± 135 |
9 | H-Box[3,4,5-(OMe)3Ph]-OMe | 317 ± 36 | 1459 ± 19 | 81 ± 5 | 878 ± 70 |
10 | H-Box[(4-OAll)Ph]-OMe | 185 ± 4 | nd | nd | nd |
11 | H-Box[(4-NMe2)Ph]-OMe | 277 ± 6 | nd | nd | nd |
12 | H-Box[(4-NPh2)Ph]-OMe | –a | nd | nd | nd |
13 | H-Box[(2-OMe-4-NMe2)Ph]-OMe | 239 ± 11 | 97 ± 3 | 29 ± 1 | 314 ± 15 |
14 | H-Box[(2-OH-4-NEt2)Ph]-OMe | 337 ± 8 | nd | nd | nd |
15 | H-Box[2,4-(OH)2Ph]-OMe | No effect | nd | nd | nd |
16 | H-Box[(4-B(OH)2)Ph]-OMe | 299 ± 8 | 627 ± 26 | 101 ± 18 | Not toxicb |
17 | H-Box[(3-B(OH)2)Ph]-OMe | 59 ± 3 | 62 ± 7 | 88 ± 15 | 672 ± 58 |
18 | H-Box[(3-OPh)Ph]-OMe | No effect | nd | nd | nd |
19 | H-Box[3,5-(CF3)2Ph]-OMe | –a | nd | nd | nd |
20 | H-Box(4-NMe2Cin)-OMe | 229 ± 5 | nd | nd | nd |
21 | H-Box(Fur)-OMe | 450 ± 10 | nd | nd | nd |
22 | H-Box(Tio)-OMe | 954 ± 44 | nd | nd | nd |
23 | H-Box(Pyrrol)-OMe | 418 ± 48 | 278 ± 32 | 110 ± 2 | 852 ± 80 |
24 | H-Box(Indol)-OMe | –a | nd | nd | nd |
25 | H-Box(Benzotio)-OMe | 79 ± 7 | 53 ± 1 | 6 ± 0.4 | 437 ± 32 |
26 | H-Box(4Py)-OMe | 1866 ± 86 | 1174 ± 21 | 112 ± 9 | 4099 ± 131 |
27 | H-Box(2Py)-OMe | 983 ± 2 | 662 ± 49 | 296 ± 9 | 1429 ± 104 |
28 | H-Box(2Q)-OMe | 131 ± 5 | 50 ± 3 | 37 ± 0.1 | 326 ± 19 |
29 | H-Box(3Q)-OMe | 299 ± 24 | 51 ± 3 | 21 ± 1 | 378 ± 18 |
30 | H-Box(3iQ)-OMe | 147 ± 3 | 58 ± 4 | 54 ± 3 | 290 ± 10 |
31 | H-Box(6Q)-OMe | –a | nd | nd | nd |
32 | H-Box(4Q)-OMe | 567 ± 20 | 106 ± 10 | 26 ± 2 | 583 ± 29 |
33 | H-Box(8Q)-OMe | 377 ± 22 | 313 ± 22 | 394 ± 9 | 198 ± 5 |
34 | H-Box(4PyBr)-OMe | 1760 ± 8 | 408 ± 3 | 73 ± 12 | 3216 ± 171 |
35 | H-Box(2PyBr)-OMe | 965 ± 44 | 234 ± 21 | 48 ± 4 | 1980 ± 112 |
36 | H-Box[(4-Me)Ph]-OH | No effect | nd | nd | nd |
37 | H-Box(BiPh)-OH | No effect | nd | nd | nd |
38 | H-Box(2-Naph)-OH | No effect | nd | nd | nd |
39 | H-Box(9-Ant)-OH | 320 ± 15 | nd | nd | nd |
40 | H-Box(2-Im)-OH | No effect | nd | nd | nd |
41 | H-Box(2-Benzofur)-OH | No effect | nd | nd | nd |
nd not determined
aToo low solubility in the conditions of the experiment
bIn the concentration range of 10–2500 μM