Table 1.
Antiproliferative activity IC50 [ng/mL] of 22a, 22c, 22e, 23c, 23f, 24b–d, 24f, 24g, 27b and 27c in comparison to AP-3 (4). Values shown are means of two determinations in parallel; human cell lines: KB-3-1 (cervix carcinoma), A-431 (epidermoid carcinoma), SK-OV-3 (ovary adenocarcinoma), PC-3 (prostate adenocarcinoma), L-929 (connective tissue of a mouse).
| cell line | KB-3-1 | A-431 | SK-OV-3 | PC-3 | L-929 |
| compound | |||||
| AP-3 4 | 0.11 | 0.050 | 0.030 | 0.035 | 0.1 |
| 22a | 2.1 | 0.31 | 0.34 | 0.26 | 4.1 |
| 22c | 0.28 | 0.65 | 3.1 | 4.0 | 78 |
| 22e | 7.5 | 5.1 | 1.8 | 0.80 | 8.7 |
| 23c | 2.2 | 0.77 | 0.46 | 0.28 | 1.9 |
| 23f | 0.38 | 0.074 | 0.099 | 0.14 | 0.81 |
| 24b | >10000 | >10000 | >10000 | >10000 | >10000 |
| 24c | 7.8 | 5.5 | 9.0 | 18 | 220 |
| 24d | 6.0 | 70 | 8.0 | 95 | 580 |
| 24f | 1800 | 2200 | 2500 | 3500 | >10000 |
| 24g | 50 | 0.85 | 70 | 3.8 | 100 |
| 27b | 2200 | >10000 | 2800 | >10000 | >10000 |
| 27c | 0.09 | 0.25 | 0.09 | 0.28 | 0.33 |