Table 1.
Cytotoxic activity data of taxol conjugates
| Cmpd | ED50 (nM)a |
ED50 (μM)
|
|||||||
|---|---|---|---|---|---|---|---|---|---|
| 1A9 | A549 | MCF-7 | LN-CAP | PC-3 | DU-145 | KB | KB-VIN | MRC-5 | |
| 1 | 1.0 | 2.3 | 1.1 | 2.6 | 55.5 | 1.3 | 1.8 | 311 | NT a |
| 2b | 739 | 1074 | 686 | 680 | 1234 | 3107 | 111.2 | 2050 | NT |
| 2d | 284.9 | 1609 | 11659 | 530.1 | 9452 | 1600 | 1365 | 14447 | >30 |
| 3a | 3.2 | 6.9 | 3.2 | 2.0 | 16.7 | 10.9 | 20.9 | 15 | NT |
| 3b | 4.3 | 12.8 | 4.3 | 4.3 | 18.4 | 7.7 | 80.6 | 25 | NT |
| 4b | 183.7 | 950.6 | 361.0 | 324.7 | 475.3 | 611.9 | 146.1 | 28977 | NT |
| 4c | 43.6 | 99.8 | 59.9 | 59.9 | 112.2 | 113.5 | 47.9 | 7426 | NT |
| 5 | >20 b | >20 b | >20 b | >20 b | >20 b | >20 b | >20 b | >20 b | NT |
| 6 | 2.9 | 10.1 | 6.4 | 4.2 | 12.1 | 8.6 | 8.4 | 9964 | >10 c |
| 7 | 8.1 | 23.7 | 22.1 | 10.2 | 42.8 | 32.5 | 13.9 | 6231 | 6174 |
| 8 | 1.6 | 2.6 | 26.7 | 3.0 | 14.8 | 3.7 | 1.3 | 62.4 | 177.7 |
| 9 | 1.5 | 2.6 | 2.7 | 1.2 | 3.1 | 2.3 | 1.9 | 2050 | 6133 |
| 10 | 1.0 | 1.9 | 34.1 | 0.34 | 19.4 | 1.9 | 1.5 | 56.3 | 243.6 |
| 11 | 10.6 | 27.3 | 26.5 | 12.9 | 50.7 | 31.9 | 19.0 | >20 b | NT |
| 12 | 10.3 | 23.2 | 24.7 | 19.5 | 71.8 | 29.8 | 17.0 | >20 b | NT |
| 13 | 14.0 | 28.5 | 29.2 | 23.7 | 70.4 | 34.4 | 21.57 | >20 b | NT |
| 14 | 2.3 | 3.8 | NT | NT | NT | NT | 5.4 | 308 | NT |
| 15 | 45.3 | 77.4 | 38.7 | 46.2 | 103.6 | 68.3 | 53.6 | >20 b | NT |
| 16 | 20.7 | 45.6 | 43.9 | 22.1 | 86.3 | 83.4 | 31.6 | >20 b | 3279 |
| 17 | 104 | 1319 | 125.0 | NT | NT | NT | 347.2 | NA | NT |
| 18 | 60.1 | 111.0 | 48.6 | 90.1 | 145.3 | 139.1 | 53.8 | 6220 | NT |
| 19 | 75.7 | 123.5 | 68.2 | 128.5 | 191.5 | 167.5 | 87.4 | 5200 | NT |
| 20 | 2.3 | 3.8 | NT | NT | NT | NT | 2.3 | 308 | NT |
| 21 | 154.3 | 224.8 | 129.8 | 192.7 | 652.1 | 311.0 | 147.3 | >20 b | NT |
Human ovarian carcinoma (1A9), human lung carcinoma (A549), breast cancer (MCF-7), human prostate carcinoma (LN-CAP, PC-3, DU-145), human umbilical vein endothelial cell (HUVEC), human epidermoid carcinoma of the nasopharynx (KB), multi-drug resistant expressing P-glycoprotein (KB-VIN) and human embryonic fibroblast (MRC-5).
a
Cytotoxicity as ED50 values for each cell line, the concentration of compound that caused 50% reduction in absorbance at 562 nm relative to untreated cells using the sulforhodamine B assay.
b
Test compound (20 μg/mL) did not reach 50% inhibition.