Table 1.
Bioactivity of paclitaxel analogs
| cmpd | tubulin polym ED50 (µM) | crit. Tb conc., µMa | Ka × 107, M−1b | A2780 cytotox IC50 (nM) | PC3 cytotox. IC50 (nM) |
|---|---|---|---|---|---|
| 1 | 0.87 ± 0.15 | 2.0 ± 0.15 | 5.48 ± 0.22 | 2.4 ± 0.2 | 4.7 ± 2.6 |
| 2c | 0.21 ± 0.09 | 0.35 ± 0.06 | NDd | 0.56 ± 0.05 | 3.1 |
| 3 | NDd | ~ 3e | <0.02 | >2000 | >8300 |
| 4 | 0.46 ± 0.08 | 0.99 + 0.18 | 8.84 ± 0.61 | 89 ± 9 | 13.8 ± 7.1 |
a
GDP-tubulin, determined as described in Supporting Information.
b
GMPcPP microtubules, determined as described in Supporting Information.
c
Data from reference 33
d
Not detemined.
e
GTP-tubulin; the value for PTX under these conditions is 0.37 µM3