Table 2.
Comparison of in vitro growth inhibition potency of epothilone derivatives against various parent and drug-resistant tumor cell lines
Compound | DC-3F | DC-3F/ADX | P388/0 | P388/Adr | SK-N-As | SK-N-FI | MCF-7 | MCF-7/Adr |
---|---|---|---|---|---|---|---|---|
IC50, μM* | ||||||||
1 | 0.0037 | 0.053 | 0.0018 | 0.0010 | 0.012 | 0.023 | 0.0030 | 0.0094 |
(14.5×) | (5.3×) | (1.9×) | (3.1×) | |||||
2 | 0.0006 | 0.017 | 0.00029 | 0.0016 | 0.004 | 0.010 | 0.0005 | 0.0027 |
(28×) | (5.5×) | (25×) | (5.4×) | |||||
3 | 0.011 | 0.042 | 0.0213 | 0.0125 | 0.073 | 0.223 | 0.032 | 0.144 |
(3.9×) | (0.59×) | (3.1×) | (4.5×) | |||||
4 | 0.00097 | 0.00091 | 0.0068 | 0.0042 | 0.021 | 0.046 | 0.0029 | 0.0071 |
(0.9×) | (0.62×) | (2.2×) | (2.4×) | |||||
Paclitaxel | 0.095 | 32.0 | 0.0029 | 0.326 | 0.0016 | 0.130 | 0.0033 | 0.150 |
(338×) | (111×) | (80×) | (46×) | |||||
Actinomycin D | 0.00044 | 0.572 | 0.00015 | 0.0012 | 0.00085 | 0.0119 | 0.00068 | 0.00167 |
(13,000×) | (8×) | (14×) | (2.5×) | |||||
Adriamycin | 0.018 | 2.236 | 0.0055 | 2.65 | 0.077 | 1.42 | 0.057 | 0.216 |
(124×) | (482×) | (18.4×) | (3.8×) |
Numbers in parentheses are folds of resistance based on the IC50 ratio when compared with the corresponding parent cell lines except for P388/0 and P388/Adr, and XTT assay (21) was used.