Table 3.
Target Compounds 3, 4, and 6–9 Circumvent Pgp and βIII-Tubulin Mediated Resistance
| IC50 ± SD (nM)
|
IC50 ± SD (nM)
|
|||||
|---|---|---|---|---|---|---|
| compd | SK-OV-3 | SK-OV-3 MDR1-M6/6 | Rr | HeLa | HeLa WTβIII | Rr |
| (±)-1·HCla (Lead) | 38.6 ± 3.1 | 44.4 ± 3.2 | 1.2 | 37.3 ± 4.1 | 23.9 ± 1.7 | 0.6 |
| 3 | 7.7 ± 0.8 | 8.4 ± 0.4 | 1.1 | 9.5 ± 0.8 | 8.1 ± 0.9 | 0.9 |
| 4 | 14.5 ± 1.0 | 18.3 ± 1.0 | 1.3 | 15.8 ± 1.4 | 14.6 ± 1.8 | 0.9 |
| 6 | 40.3 ± 2.6 | 71.0 ± 19 | 1.8 | 33.8 ± 7.4 | 35.3 ± 9.9 | 1.0 |
| 7 | 147.8 ± 2.9 | 200.0 ± 17.1 | 1.4 | 111.1 ± 19.0 | 115.9 ± 9.8 | 1.0 |
| 8 | 155.8 ± 15.0 | 161.9 ± 21.5 | 1.0 | 120.5 ± 4.2 | 159.0 ± 17.6 | 1.3 |
| 9 | 18.6 ± 0.1 | 32.1 ± 1.5 | 1.7 | 15.7 ± 1.2 | 14.9 ± 1.9 | 0.9 |
| paclitaxel | 5.0 ± 0.6 | 1,200 ± 58 | 240 | 2.8 ± 0.36 | 24.0 ± 3.0 | 8.6 |
| CA-4 | 5.5 ± 0.5 | 7.2 ± 1.1 | 1.3 | 3.3 ± 0.4 | 3.3 ± 0.3 | 1.0 |
Results previously published.25