Table 1.
Antiproliferative activity of compounds 1–82 against A375, MDA-MB-231, SMMC-7721, SGC-7901 and MGC-803 cell lines.a
| Compound | IC50 (μM) |
||||
|---|---|---|---|---|---|
| A375 | MDA-MB-231 | SMMC-7721 | SGC-7901 | MGC-803 | |
| 1 | 5.21 ± 0.39 | 8.67 ± 0.61 | -b | – | – |
| 2 | 22.79 ± 0.71 | 58.56 ± 1.78 | 28.53 ± 1.47 | – | 28.58 ± 1.27 |
| 3 | 27.01 ± 0.82 | 31.83 ± 1.44 | – | – | – |
| 4 | 16.90 ± 1.22 | 24.72 ± 2.15 | 73.79 ± 1.70 | – | – |
| 5 | 5.84 ± 0.33 | 8.39 ± 0.89 | 4.05 ± 0.20 | 32.88 ± 1.85 | – |
| 6 | 5.99 ± 0.49 | 9.20 ± 1.27 | 15.86 ± 0.35 | – | 44.19 ± 1.25 |
| 7 | 9.84 ± 0.78 | 12.26 ± 0.64 | 13.34 ± 0.39 | – | 12.91 ± 0.30 |
| 8 | 9.12 ± 0.82 | 17.47 ± 1.77 | 10.72 ± 0.80 | – | 17.21 ± 0.41 |
| 9 | 24.05 ± 0.99 | 36.52 ± 2.56 | 9.04 ± 0.99 | – | 38.64 ± 1.22 |
| 10 | 5.43 ± 0.40 | 29.78 ± 2.31 | 40.10 ± 1.66 | – | 24.93 ± 0.82 |
| 11 | 10.59 ± 0.90 | 5.66 ± 0.28 | 65.77 ± 1.79 | – | – |
| 12 | 3.58 ± 0.11 | 4.25 ± 0.32 | – | – | – |
| 13 | – | – | – | – | – |
| 14 | 49.97 ± 1.78 | 3.60 ± 0.30 | 26.97 ± 1.01 | – | – |
| 15 | 13.06 ± 0.70 | 3.64 ± 0.22 | – | – | – |
| 16 | 21.14 ± 0.87 | 28.47 ± 1.78 | 45.56 ± 1.29 | – | – |
| 17 | 12.06 ± 1.19 | 10.55 ± 0.91 | – | – | – |
| 18 | 3.82 ± 0.31 | 5.24 ± 0.40 | 24.80 ± 1.58 | – | – |
| 19 | 20.13 ± 0.90 | 12.09 ± 1.52 | – | – | – |
| 20 | 10.43 ± 0.82 | 3.18 ± 0.20 | 20.04 ± 1.74 | – | – |
| 21 | 16.60 ± 0.91 | 23.14 ± 2.78 | 11.77 ± 0.60 | 30.76 ± 2.00 | – |
| 22 | 4.14 ± 0.21 | 6.54 ± 0.74 | 26.12 ± 0.73 | – | – |
| 23 | 25.31 ± 1.33 | 33.75 ± 2.89 | – | – | – |
| 24 | 24.49 ± 1.55 | 41.84 ± 2.97 | 52.75 ± 1.44 | – | – |
| 25 | – | – | – | – | – |
| 26 | – | – | – | – | – |
| 27 | 7.83 ± 0.40 | 39.80 ± 2.55 | 50.66 ± 1.82 | – | – |
| 28 | 10.15 ± 0.75 | 20.55 ± 2.11 | 16.70 ± 0.65 | – | – |
| 29 | 14.34 ± 0.91 | 16.92 ± 0.87 | – | – | – |
| 30 | 27.99 ± 1.31 | 25.09 ± 0.99 | 2.29 ± 0.17 | – | – |
| 31 | 3.49 ± 0.20 | 24.08 ± 1.18 | 33.48 ± 0.88 | – | – |
| 32 | 12.28 ± 0.41 | 16.15 ± 0.41 | 27.02 ± 0.90 | – | – |
| 33 | 4.96 ± 0.51 | 19.04 ± 0.65 | 26.20 ± 0.39 | – | 35.88 ± 0.79 |
| 34 | 5.37 ± 0.60 | 23.39 ± 0.88 | 22.99 ± 0.45 | – | – |
| 35 | 7.41 ± 0.77 | 7.41 ± 0.33 | 36.45 ± 0.70 | – | – |
| 36 | 4.01 ± 0.68 | 37.17 ± 1.40 | 28.98 ± 0.78 | – | – |
| 37 | 9.09 ± 0.81 | 21.48 ± 1.29 | 35.11 ± 0.49 | – | – |
| 38 | 40.81 ± 1.39 | 83.15 ± 2.91 | – | – | – |
| 39 | – | – | – | – | – |
| 40 | 6.73 ± 0.50 | 18.34 ± 0.80 | 35.61 ± 0.55 | 51.30 ± 2.55 | – |
| 41 | 14.55 ± 1.20 | 10.57 ± 0.46 | 28.80 ± 0.75 | – | – |
| 42 | – | – | – | – | – |
| 43 | 38.60 ± 0.61 | 43.99 ± 1.20 | 34.48 ± 0.77 | 24.75 ± 0.89 | – |
| 44 | 5.34 ± 0.30 | – | 9.24 ± 0.40 | – | – |
| 45 | 8.61 ± 0.28 | – | 15.59 ± 0.78 | – | – |
| 46 | 1.25 ± 0.07 | – | 5.37 ± 0.11 | – | – |
| 47 | 9.04 ± 0.29 | 10.25 ± 0.44 | 21.15 ± 0.49 | – | – |
| 48 | 27.41 ± 1.50 | 39.70 ± 1.39 | 50.96 ± 1.91 | 49.14 ± 1.39 | – |
| 49 | 32.76 ± 1.44 | 35.23 ± 1.40 | 48.49 ± 1.65 | 49.79 ± 0.47 | – |
| 50 | 20.69 ± 1.39 | 31.56 ± 1.20 | 29.09 ± 1.27 | 26.89 ± 0.56 | – |
| 51 | 42.04 ± 1.60 | 20.87 ± 1.09 | 31.25 ± 1.33 | – | – |
| 52 | 13.29 ± 0.87 | 15.29 ± 0.82 | 24.30 ± 1.19 | – | – |
| 53 | 17.49 ± 0.98 | 28.48 ± 1.14 | 57.32 ± 2.01 | – | – |
| 54 | 17.52 ± 1.52 | 28.51 ± 1.16 | 19.03 ± 0.71 | – | – |
| 55 | 5.87 ± 0.20 | 14.31 ± 1.07 | 34.10 ± 1.45 | – | – |
| 56 | 6.92 ± 0.44 | 12.16 ± 0.92 | 19.31 ± 0.82 | 34.46 ± 1.04 | – |
| 57 | 1.58 ± 0.06 | 3.22 ± 0.18 | – | – | – |
| 58 | – | – | – | – | – |
| 59 | 57.98 ± 1.71 | – | – | – | – |
| 60 | 10.70 ± 0.80 | – | – | – | – |
| 61 | 27.30 ± 1.00 | 26.87 ± 1.20 | 28.20 ± 1.49 | – | 27.06 ± 1.03 |
| 62 | 45.13 ± 1.40 | 86.18 ± 2.44 | – | – | – |
| 63 | – | – | – | – | – |
| 64 | 23.87 ± 1.37 | 38.29 ± 0.90 | – | – | – |
| 65 | 32.68 ± 1.22 | 30.53 ± 1.29 | – | – | – |
| 66 | 8.56 ± 0.49 | 30.29 ± 1.22 | 51.96 ± 1.70 | – | 19.59 ± 1.17 |
| 67 | 8.29 ± 0.42 | 12.07 ± 0.37 | 15.04 ± 0.60 | 50.26 ± 1.17 | 16.13 ± 0.82 |
| 68 | 19.65 ± 1.00 | 21.25 ± 0.80 | – | – | 37.41 ± 1.35 |
| 69 | 8.79 ± 0.61 | 7.95 ± 0.40 | 11.52 ± 0.39 | 36.82 ± 1.25 | 25.09 ± 0.54 |
| 70 | 3.09 ± 0.19 | 4.22 ± 0.20 | 3.00 ± 0.18 | 5.38 ± 0.30 | 3.15 ± 0.27 |
| 71 | 8.65 ± 0.33 | 8.09 ± 0.52 | 23.18 ± 0.78 | – | 20.80 ± 0.79 |
| 72 | 12.98 ± 0.77 | 22.55 ± 1.00 | 16.05 ± 0.91 | – | 44.91 ± 1.13 |
| 73 | 11.16 ± 0.81 | 25.58 ± 0.97 | – | – | 57.70 ± 1.44 |
| 74 | 26.79 ± 1.22 | 34.72 ± 1.20 | – | 31.83 ± 0.82 | 35.31 ± 1.25 |
| 75 | 9.27 ± 0.91 | 21.34 ± 1.04 | 32.07 ± 1.02 | 21.93 ± 0.61 | – |
| 76 | 18.00 ± 1.09 | 36.02 ± 1.20 | – | 50.20 ± 1.79 | – |
| 77 | 13.68 ± 1.29 | 19.44 ± 0.79 | 23.61 ± 1.45 | – | 51.81 ± 0.87 |
| 78 | 26.26 ± 2.35 | 35.22 ± 1.28 | – | – | – |
| 79 | 22.97 ± 1.75 | – | – | – | – |
| 80 | – | – | – | 26.81 ± 1.01 | – |
| 81 | 7.89 ± 0.56 | 27.77 ± 1.32 | 34.92 ± 1.70 | – | – |
| 82 | 24.16 ± 0.60 | 28.67 ± 1.21 | 8.95 ± 0.27 | – | – |
| AMD | 0.52 ± 0.14 | 0.81 ± 0.11 | 1.05 ± 0.09 | 0.92 ± 0.08 | 0.67 ± 0.08 |
a
The standard deviation (SD) of three time independent tests.
b
The standard deviation (SD) of three time independent tests.