Table 1.
Bioactivity data for all synthesized compounds.
| Compound number |
Modified Site |
NF-κB SEAPa Compound alone |
MTTb Compound alone |
||
|---|---|---|---|---|---|
| % Activation |
SEM | % Viability |
SEM | ||
| 1 | -- | 200 | - | 103 | 3.3 |
| 12b | A | 100 | 0.2 | 98 | 1.8 |
| 12c | A | 100 | 0.3 | 98 | 1.7 |
| 12d | A | 254 | 12.2 | 98 | 3.0 |
| 12e | A | 207 | 15.9 | 91 | 5.8 |
| 12f | A | 101 | 0.2 | 100 | 3.5 |
| 12g | A | 100 | 0.3 | 108 | 5.5 |
| 12h | A | 100 | 0.7 | 120 | 7.9 |
| 12i | A | 100 | 0.6 | 115 | 6.6 |
| 12j | A | 101 | 0.5 | 116 | 5.5 |
| 12k | A | 99 | 0.4 | 113 | 7.5 |
| 12l | A | 179 | 12.5 | 103 | 5.4 |
| 12m | A | 98 | 0.4 | 102 | 3.3 |
| 12n | A | 98 | 0.5 | 98 | 4.9 |
| 12o | A | 97 | 0.8 | 91 | 4.2 |
| 12p | A | 185 | 4.5 | 100 | 6.1 |
| 12q | A | 198 | 7.9 | 93 | 4.4 |
| 12r | A | 109 | 3.2 | 89 | 4.3 |
| 12s | A | 114 | 7.8 | 95 | 4.6 |
| 12t | A | 101 | 0.6 | 92 | 6.0 |
| 12u | A | 203 | 5.7 | 102 | 1.2 |
| 18a | B | 99 | 0.9 | 51 | 0.6 |
| 18b | B | 100 | 1.2 | 94 | 1.7 |
| 18c | B | 100 | 0.8 | 93 | 2.9 |
| 18d | B | 100 | 0.8 | 93 | 2.0 |
| 18e | B | 99 | 0.4 | 101 | 1.7 |
| 18f | B | 100 | 0.2 | 90 | 5.7 |
| 18g | B | 99 | 0.5 | 94 | 5.0 |
| 18h | B | 99 | 0.4 | 89 | 2.4 |
| 18i | B | 99 | 0.4 | 98 | 4.0 |
| 18j | B | 100 | 1.2 | 106 | 3.1 |
| 18k | B | 103 | 0.9 | 102 | 5.9 |
| 18l | B | 102 | 1.0 | 104 | 3.6 |
| 18m | B | 159 | 7.2 | 97 | 7.8 |
| 18n | B | 133 | 3.2 | 84 | 3.0 |
| 18o | B | 118 | 5.3 | 111 | 6.2 |
| 18p | B | 264 | 14.7 | 103 | 3.1 |
| 18q | B | 393 | 12.2 | 106 | 3.9 |
| 18r | B | 179 | 12.2 | 104 | 3.1 |
| 18s | B | 109 | 3.7 | 129 | 7.7 |
| 18t | B | 117 | 4.3 | 108 | 3.2 |
| 34a | C | 99 | 0.9 | 85 | 2.7 |
| 34b | C | 99 | 0.8 | 91 | 1.7 |
| 34c | C | 101 | 1.0 | 97 | 3.8 |
| 34d | C | 100 | 0.3 | 102 | 4.6 |
| 42a | D | 99 | 0.7 | 94 | 1.2 |
| 42b | D | 100 | 1.1 | 89 | 2.0 |
| 42c | D | 103 | 1.6 | 97 | 5.8 |
| 42d | D | 223 | 8.9 | 88 | 2.3 |
| 42e | D | 209 | 9.2 | 90 | 1.7 |
| 42f | D | 115 | 2.5 | 93 | 1.2 |
| 42g | D | 99 | 1.0 | 99 | 2.8 |
| 42h | D | 127 | 4.0 | 87 | 2.3 |
| 42i | D | 120 | 4.6 | 96 | 2.5 |
| 42j | D | 99 | 1.9 | 99 | 2.5 |
| 42k | D | 125 | 2.5 | 92 | 2.5 |
| 45a | E | 100 | 0.5 | 85 | 2.5 |
| 45b | E | 100 | 0.8 | 82 | 2.2 |
| 45c | E | 99 | 0.6 | 88 | 0.8 |
| 45d | E | 100 | 0.5 | 88 | 2.9 |
| 51 | C,E | 103 | 1.1 | 69 | 6.4 |
| 54a | F | 183 | 11.0 | 104 | 15.7 |
| 54b | F | 167 | 19.0 | 96 | 4.3 |
| 54c | F | 102 | 0.9 | 101 | 6.9 |
| 54d | F | 105 | 2.5 | 81 | 2.3 |
| 54e | F | 100 | 0.9 | 91 | 4.0 |
| 54f | F | 101 | 0.8 | 132 | 3.6 |
| 54g | F | 201 | 4.7 | 117 | 6.6 |
| 54h | F | 517 | 34.8 | 111 | 7.1 |
| 54i | F | 101 | 0.7 | 121 | 0.3 |
| 54j | F | 101 | 0.5 | 114 | 4.9 |
| 54k | F | 100 | 0.7 | 80 | 13.5 |
| 55 | A,F | 191 | 4.4 | 97 | 2.9 |
| 57 | B,F | 112 | 3.0 | 102 | 1.9 |
| 60 | A,B | 202 | 3.4 | 95 | 2.4 |
| 61 | A,B,F | 111 | 0.7 | 97 | 2.4 |
a
The % activation values in NF-κB SEAP assay for compounds were two point normalized between compound 1 as 200% and Vehicle (0.5% DMSO) as 100%. The mean SEAP response in NF-κB assay for compound 1 and DMSO was 0.4 ± 0.02 and 0.033 ± 0.001 μg/mL, respectively.
b
The % viability values for compounds in MTT assay was normalized to DMSO as 100%. The mean OD value at 405 nm for DMSO was 1.14 ± 0.01. All the compounds were evaluated at 5μM concentration. All raw values used for normalization are represented as mean ± SEM.