Table 1.
Cytotoxic Activity Data for 1-Analogs
| ED50 (μg/mL)a | ||||||||
|---|---|---|---|---|---|---|---|---|
| Cmpd | A549 | A431 | 1A9 | HCT-8 | PC-3 | KB | KB-VIN | HUVEC |
| 1 | 3.5 | 5.1 | 3.5 | 3.7 | 11.1 | 4.0 | 3.0 | 2.1 |
| 2 | 1.4 | 9.0 | 1.1 | 7.4 | 17.7 | 1.7 | 1.9 | 3.6 |
| 3 | 3.0 | 9.2 | 2.8 | 5.6 | 18.2 | 3.6 | 2.9 | 2.5 |
| 4 | 2.8 | 4.5 | 2.9 | 2.9 | 14.3 | 3.3 | 2.4 | 1.6 |
| 5 | 2.4 | 6.6 | 2.5 | 4.1 | 15.6 | 3.3 | 2.8 | 1.7 |
| 6 | 3.1 | 14.9 | 2.9 | 14.8 | NAb | 3.8 | 3.8 | 4.0 |
| 7 | 3.3 | 4.1 | NTC | 3.6 | 7.2 | 3.7 | 2.7 | 2.0 |
| 8 | 4.3 | 5.1 | NT | 4.1 | 8.2 | 3.9 | 1.9 | 2.4 |
| 9 | 4.6 | 5.2 | NT | 4.0 | 9.0 | 4.1 | 1.6 | 2.3 |
| 10 | 6.1 | 12.0 | 5.3 | 10.5 | 15.1 | 6.9 | 1.9 | NT |
| 11 | 8.3 | 10.1 | NT | 7.8 | 17.1 | 7.1 | 2.1 | 3.0 |
| 12 | 4.3 | 4.0 | NT | 2.9 | 8.8 | 3.1 | 1.6 | 2.5 |
| 13 | 8.0 | 20.0 | 6.2 | 8.4 | NA | NA | 1.84 | NT |
| 14 | 2.2 | 2.6 | NT | 2.1 | 4.6 | 1.9 | 1.1 | 1.1 |
| 15 | 3.6 | 4.1 | NT | 2.3 | 9.0 | 2.8 | 1.3 | 1.8 |
| 16 | 10.0 | 14.7 | 7.9 | 17.5 | 20.6 | 9.9 | 8.8 | 2.4 |
| 17 | 4.5 | 10.8 | 4.0 | 8.6 | 18.2 | 5.5 | 3.4 | 2.5 |
| 18 | 3.5 | 6.0 | 3.5 | 5.1 | 10.8 | 4.3 | 3.0 | 1.6 |
| 19 | >5 | 10.5 | 4.6 | 5.0 | 11.1 | 7.3 | 3.8 | 2.0 |
| 20 | >5(48) | 7.0 | 3.6 | 3.3 | 14.2 | 4.1 | 2.9 | NA |
| 21 | 5.5 | 13.8 | 3.8 | 9.4 | 18.9 | 4.3 | 0.3 | NT |
| 22 | 3.4 | 5.4 | 2.1 | 2.8 | 7.7 | 2.8 | 1.2 | NT |
| 23 | 4.6 | 10.3 | 4.3 | 9.4 | 15.0 | 3.0 | 1.0 | NT |
| 24 | 3.8 | 9.8 | 3.8 | 8.5 | 15.0 | 3.6 | 2.6 | NT |
| 25 | 1.4 | 1.9 | 1.5 | 1.4 | 3.3 | 0.6 | 0.8 | NT |
| 26 | 1.0 | 1.2 | 0.9 | 1.3 | 2.3 | 0.9 | 0.9 | NT |
| 27 | 9.0 | 14.0 | 8.0 | 15.8 | 17.8 | 10.5 | 6.5 | 2.1 |
a
See Experimental “Cytotoxic Activity Assay” for cell line descriptions.
b
Not active: >20 μg/mL
c
Not tested.