Antiproliferative activity of the 3,3-disubstituted-6,6-pentamethylene-1,5-diazabicyclo[3.1.0]hexane-2,4-diones in derived suspended tumor cell lines
| ED50 Values1-160 | ||||||||
|---|---|---|---|---|---|---|---|---|
| Compounds | Murine | Human | ||||||
| L1210 | P388 | THP1 | Tmolt3 | Tmolt4 | HUT-78 | HL-60 | HeLa S3 | |
| 1 | 2.49 | 1.54 | 2.71 | 1.74 | 0.80 | 1.81 | 1.01 | 2.21 |
| (10.5) | (6.5) | (11.4) | (7.3) | (3.3) | (7.6) | (4.2) | (9.3) | |
| 2 | 2.82 | 2.23 | 2.50 | 3.01 | 2.29 | 2.75 | 3.89 | 2.42 |
| (9.9) | (7.8) | (8.7) | (10.5) | (8.0) | (9.6) | (13.6) | (8.5) | |
| 3 | 2.65 | 2.72 | 4.94 | 2.65 | 2.48 | 3.50 | 4.70 | 3.58 |
| (8.8) | (9.1) | (16.5) | (8.8) | (8.3) | (11.7) | (15.7) | (11.9) | |
| 6-MP | 2.43 | 2.04 | 3.03 | 1.62 | 2.67 | 1.63 | 3.35 | 2.12 |
| (14.3) | (12.0) | (17.8) | (9.5) | (15.7) | (9.6) | (19.7) | (12.4) | |
| VP-16 | 1.83 | 0.99 | 3.27 | 1.00 | 1.92 | 1.33 | 4.43 | 1.89 |
| (3.1) | (1.7) | (5.6) | (1.7) | (3.3) | (2.3) | (7.5) | (3.2) | |
| MPA | 2.32 | 0.92 | 2.29 | 2.44 | 2.86 | 1.63 | 4.27 | 1.47 |
| (7.2) | (2.9) | (7.1) | (7.6) | (8.9) | (5.1) | (13.3) | (4.6) | |
ED50 values are expressed as μg/ml (μM) and were calculated as the mean of four independent experiments. ED50 values of <4 μg/ml were required for significant growth inhibition by National Institutes of Health standards. Incubations were conducted with 5 × 104 cells in a final volume of 1 ml for 72 h at 37°C in a 5% CO2 atmosphere.
↵1-160 p < 0.01.