Table 7.
Anti-proliferative activity of selected analogues against melanoma and HNSCC.
| Compound (IC50, µM) |
B16F10 | SKMEL28 | MDA1986 | JMAR |
|---|---|---|---|---|
| 6b | 5.77 ± 0.96a | 12.40 ± 0.64a | 6.70 ± 1.20a | 24.60 ± 1.92a |
| 12a | 2.30 ± 0.32 | 2.14 ± 0.08 | 1.67 ± 0.16 | 12.60 ± 0.40 |
| 14a | 37.50 ± 6.56 | 14.90 ± 2.88 | 13.40 ± 4.24 | 2.79 ± 0.64 |
| 15a | 8.56 ± 2.16 | 15.80 ± 0.48 | 3.70 ± 0.64 | 6.14 ± 1.28 |
| 17a | 1.01 ± 0.48 | 1.47 ± 0.24 | 0.81 ± 0.40 | 16.10 ± 2.16 |
| 18a | 10.40 ± 1.20 | 19.60 ± 2.48 | 18.80 ± 3.68 | 3.60 ± 0.40 |
| 23a | 9.60 ± 1.12 | 10.65 ± 0.40 | 5.70 ± 0.56 | 5.80 ± 1.04 |
| 25a | 4.55 ± 1.20 | 5.74 ± 2.08 | 1.94 ± 0.40 | 12.64 ± 1.28 |
| 25b | 1.30 ± 0.16 | 6.41 ± 0.56 | 5.73 ± 0.96 | 2.71 ± 0.32 |
| 27a | 42.70 ± 3.36 | 18.40 ± 2.96 | 21.40 ± 3.12 | 14.90 ± 3.68 |
| 30a | 12.70 ± 1.44 | 21.40 ± 3.28 | 6.90 ± 2.08 | 24.10 ± 3.28 |
| 31a | 9.37 ± 1.04 | 12.40 ± 2.48 | 18.80 ± 3.76 | 6.19 ± 2.48 |
| 33a | >50 | 18.50 ± 5.76 | 22.90 ± 4.96 | 7.40 ± 1.68 |
| 40a | >50 | 23.80 ± 2.88 | 24.40 ± 2.00 | 6.70 ± 2.32 |
| 41a | >50 | 20.60 ± 2.16 | 21.80 ± 4.32 | 24.90 ± 2.80 |
| 42a | >50 | 18.60 ± 2.00 | 22.40 ± 3.36 | 7.50 ± 1.84 |
| 43a | 15.90 ± 2.16 | 3.47 ± 1.20 | 18.80 ± 0.64 | 8.50 ± 1.68 |
| 44a | 2.50 ± 0.48 | 11.41 ± 1.28 | 6.74 ± 2.08 | 2.73 ± 0.32 |
| 45a | 14.10 ± 2.08 | 2.94 ± 1.20 | 17.90 ± 1.44 | 13.90 ± 2.00 |
| 48a | 2.94 ± 0.08 | 5.41 ± 0.08 | 6.54 ± 0.56 | 3.40 ± 0.16 |
| 48b | 3.41 ± 0.32 | 5.49 ± 1.12 | 5.97 ± 0.40 | 6.71 ± 0.24 |
| 48c | 2.86 ± 0.24 | 5.41 ± 0.16 | 5.90 ± 0.40 | 11.60 ± 0.32 |
| 50c | 21.40 ± 1.28 | 27.60 ± 1.20 | 25.10 ± 2.08 | 35.10 ± 1.20 |
| 51a | 6.40 ± 1.92 | 10.79 ± 0.64 | 7.70 ± 0.56 | 11.40 ± 1.20 |
| 51b | 6.47 ± 2.80 | 1.48 ± 0.48 | 2.36 ± 0.08 | 1.94 ± 0.16 |
| 51c | 6.14 ± 0.64 | 31.50 ± 1.84 | 16.40 ± 1.68 | 18.40 ± 2.56 |
| 52a | 2.80 ± 0.40 | 6.14 ± 1.28 | 5.60 ± 1.04 | 5.89 ± 0.48 |
| 52b | 11.75 ± 0.40 | 11.40 ± 2.56 | 21.70 ± 1.12 | 11.60 ± 1.92 |
| 52c | 5.04 ± 0.32 | 13.80 ± 2.56 | 13.80 ± 3.44 | 11.50 ± 0.72 |
| 53a | 12.40 ± 2.00 | 20.9 ± 2.56 | 22.40 ± 1.36 | 15.14 ± 1.84 |
| 53c | 23.90 ± 2.88 | 29.40 ± 3.36 | 36.40 ± 1.20 | 32.80 ± 3.36 |
| 55b | 6.58 ± 0.48 | 5.90 ± 1.68 | 5.90 ± 0.48 | 6.70 ± 0.24 |
| 55c | 2.81 ± 0.32 | 5.73 ± 0.32 | 12.80 ± 1.28 | 24.50 ± 0.72 |
| 57a | 1.90 ± 0.24 | 2.79 ± 0.96 | 23.60 ± 2.88 | >50 |
| 57b | 0.64 ± 0.08 | 14.67 ± 0.40 | 12.80 ± 1.92 | 12.70 ± 1.44 |
| 57c | 1.84 ± 0.08 | 7.19 ± 0.24 | 6.40 ± 0.96 | 5.70 ± 0.32 |
| 59a | 2.76 ± 0.32 | 5.19 ± 0.16 | 2.74 ± 0.08 | 5.91 ± 0.40 |
| 59b | 2.14 ± 0.08 | 16.45 ± 1.36 | 10.90 ± 0.64 | 12.60 ± 0.32 |
| 59c | 1.84 ± 0.16 | 5.75 ± 0.24 | 14.60 ± 1.20 | 10.90 ± 0.48 |
| 60a | 2.60 ± 0.32 | 6.14 ± 0.56 | 4.50 ± 0.08 | 12.60 ± 0.32 |
| 60b | 1.51 ± 0.24 | 7.14 ± 0.40 | 11.40 ± 2.56 | 7.50 ± 0.64 |
| 60c | 2.67 ± 0.32 | 5.86 ± 1.20 | 13.20 ± 0.72 | 19.10 ± 2.56 |
| 61b | 0.41 ± 0.08 | 6.14 ± 0.32 | 13.10 ± 1.68 | 13.10 ± 0.64 |
| 61c | 36.73 ± 0.64 | 3.74 ± 0.24 | 1.54 ± 0.08 | 1.84 ± 0.08 |
| 64a | 37.40 ± 2.16 | 25.60 ± 2.96 | 21.90 ± 2.56 | 35.10 ± 2.16 |
| 65a | 15.70 ± 4.56 | 14.70 ± 1.92 | 17.50 ± 3.28 | 18.40 ± 2.00 |
| 78c | 1.19 ± 0.32 | 1.47 ± 0.08 | 1.42 ± 0.16 | 1.24 ± 0.24 |
| 82c | 2.03 ± 0.08 | 1.35 ± 0.08 | 1.81 ± 0.32 | 2.65 ± 0.24 |
a
Values represent mean ± standard deviation for at least two separate experiments performed in triplicate.