Table 1.
Biochemical properties of cytotoxic conjugates. The IC50’s for inhibition of purified ovine COX-1, mouse COX-2, or COX-2 in 1483 HNSCC cell line.
| |||||
|---|---|---|---|---|---|
|
| |||||
| No | R1 | R2 | Purified Enzyme IC50 (μM) |
1483 Cells IC50 (μM) |
|
| COX-1 | COX-2 | COX-2 | |||
| 1 | - | I | > 25 | > 25 | NT |
| 2 |
|
I | > 25 | > 25 | NT |
| 3 |
|
I | > 25 | 2.20 | NT |
| 4 |
|
I | > 25 | 0.25 | 0.42 |
| 5 |
|
II | > 25 | 0.45 | 0.98 |
| 6 |
|
III | > 25 | 0.10 | NT |
| 7 |
|
IV | > 25 | 0.60 | NT |
| 8 |
|
V | > 25 | 0.92 | NT |
| 9 |
|
V | > 25 | > 25 | NT |
| 10 |
|
VI | > 25 | > 25 | NT |
| 11 |
|
VII | > 25 | > 47 | NT |
| 12 |
|
VII | > 25 | 0.29 | 0.20 |
| 13 |
|
VII | > 25 | 0.25 | NT |
| 14 |
|
VII | > 25 | 0.14 | NT |
| 15 |
|
VII | > 25 | 0.18 | NT |
| 16 |
|
VIII | > 25 | 0.48 | 0.20 |
| - | Podophyllotoxin | - | > 25 | > 25 | NT |
| - | Indomethacin | - | 0.05 | 0.75 | NT |