Table 5.
Cytotoxicity of second-generation taxoids with modifications at C1O (IC50 nM)a
![]() | ||||
|---|---|---|---|---|
| Taxoid | R | LCC6-WTb | LCC6-MDRc | R/S |
| Paclitaxel | -- | 3.1 | 346 | 112 |
| 6a | Bz | 1.8 | 4.8 | 2.7 |
| 6b | ![]() |
2.1 | 5.8 | 2.7 |
| 6c | ![]() |
2.8 | 5.1 | 1.8 |
| 6d | ![]() |
3.8 | 4.7 | 1.2 |
| 6e | ![]() |
2.1 | 5.7 | 2.7 |
| 6f | ![]() |
5.3 | 15.2 | 2.9 |
| 6g | ![]() |
6.3 | 15.2 | 2.4 |
| 6h | Cbz | 1.8 | 16.7 | 9.3 |
| 6i | ![]() |
2.3 | 13.8 | 6.0 |
| 6j | ![]() |
2.1 | 20.3 | 9.7 |
| 6k | ![]() |
1.4 | 38.4 | 27.4 |
| 6l | ![]() |
5.1 | 31.2 | 6.1 |
| 6m | ![]() |
1.5 | 5.0 | 3.3 |
| 6n | ![]() |
3.7 | 6.7 | 1.8 |
| 6o | ![]() |
1.7 | 4.9 | 2.9 |
Concentration of compound which inhibits 50% (IC50, nM) of the growth of human tumor cell line after 72 h drug exposure.
LCC6-WT: human breast carcinoma cell line (Pgp−).
LCC6-MDR: mdrl transduced cell line (Pgp+).
Resistance factor = (IC50 for drug resistant cell line, R)/(IC50 for drug-sensitive cell line, S).













