Table 1.
In vitro inhibitory effects of compounds 3a–b, 4a–ac and CA4 against the proliferation of murine leukemia (L1210), murine mammary carcinoma (FM3A), human T-lymphocyte (Molt/4 and CEM) and human cervix carcinoma (HeLa) cells
| Compound | IC50 (nM)a | ||||
|---|---|---|---|---|---|
| L1210 | FM3A/0 | Molt4/C8 | CEM/0 | Hela | |
| 4a | >10,000 | >10,000 | 8000 ± 100 | >10,000 | 7900 ± 100 |
| 4b | 410 ± 23 | 550 ± 42 | 360 ± 10 | 870 ± 50 | 410 ± 16 |
| 4c | >10,000 | >10,000 | 9400 ± 500 | >10,000 | >10,000 |
| 4d | 90 ± 2 | 100 ± 10 | 59 ± 12 | 70 ± 21 | 110 ± 20 |
| 4e | >10,000 | >10,000 | 7800 ± 290 | >10,000 | >10,000 |
| 4f | 7100 ± 580 | 8400 ± 300 | 2500 ± 160 | 7200 ± 210 | >10 |
| 4g | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| 4h | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| 4i | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| 4j | 1800 ± 400 | 1200 ± 400 | 770 ± 20 | 1900 ± 400 | 570 ± 110 |
| 4k | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| 4l | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| 4m | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| 4n | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| 4o | 2100 ± 200 | 2100 ± 10 | 1300 ± 80 | 2000 ± 50 | 890 ± 130 |
| 4p | 590 ± 40 | 570 ± 30 | 200 ± 70 | 490 ± 10 | 340 ± 30 |
| 4q | 2300 ± 400 | 4400 ± 390 | 1900 ± 100 | 400 ± 150 | 1900 ± 200 |
| 4r | 24 ± 0 | 27 ± 7 | 19 ± 2 | 20 ± 2 | 3.2 ± 0.6 |
| 4s | 1700 ± 400 | 1700 ± 100 | 400 ± 30 | 2400 ± 150 | 530 ± 28 |
| 4t | 2.0 ± 1.2 | 2.8 ± 1.0 | 1.2 ± 0.8 | 2.8 ± 0.6 | 6.3 ±2.7 |
| 4u | 3500 ± 200 | 3700 ± 100 | 2100 ± 0 | 2700 ± 200 | 2000 ± 0 |
| 4v | 480 ± 32 | 330 ± 10 | 84 ± 21 | 100 ± 10 | 130 ± 24 |
| 4w | 800 ± 31 | 430 ± 27 | 240 ± 30 | 430 ± 0 | 290 ± 10 |
| 4x | >10,000 | >10,000 | 1300 ± 90 | 4300 ± 300 | 260 ± 16 |
| 4y | 180 ± 0 | 320 ± 40 | 100 ± 10 | 220 ± 80 | 100 ± 25 |
| 4z | >10,000 | 7009 ± 530 | 3005 ± 120 | >10,000 | >10,000 |
| 4aa | >10,000 | >10,000 | >10,000 | >10,000 | 4400 ± 290 |
| 4ab | 2300 ± 400 | 2600 ± 600 | 770 ± 43 | 1500 ± 300 | 680 ± 10 |
| 4ac | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 |
| 3a | 430 ± 40 | 280 ± 160 | 140 ± 20 | 87 ± 22 | n.d. |
| 3b | 65 ± 5 | 59 ± 5 | 48 ± 4 | 78 ± 3 | n.d. |
| CA4 | 2.8 ± 1.1 | 42 ± 6.0 | 16 ± 1.4 | 1.9 ± 1.6 | 1.9 ± 1.6 |
n.d. = not determined.
a
IC50 = Compound concentration required to inhibit tumor cell proliferation by 50%. Data are expressed as the mean ± SE from the dose–response curves of at least three independent experiments.